As gold catalysts have the advantages of high reactivity, unique selectivity, and high affinity for π bonds, they are usually used to activate alkynes, alkenes, and allenes. Gold catalysts not only promote the activation of alkynes to form vinyl gold intermediates or gold carbene intermediates to participate in the reaction, but also catalyze the intramolecular cyclization to form new types of heterocycles or polycyclic compounds. This review summarizes the gold-catalyzed intramolecular cyclization of alkynes in recent eight years, including the intramolecular cyclization of different nucleophilic carbon-atom and heteroatoms, and its applications in the total synthesis of natural products.

As third-generation cyclin-dependent kinase inhibitors, CDK4/6 inhibitors have become pivotal therapeutic agents in the treatment of breast cancer, lung cancer, and other malignancies due to their favorable safety profile and high in vivo efficacy. This review provides a systematic examination of the synthetic routes of eight representative compounds—palbociclib and dalpiciclib, ribociclib and volbociclib, abemaciclib and tericiclib, as well as trilaciclib and lerociclib—selected based on their time of market authorization and structural homology. Special emphasis is placed on the role of novel reaction systems and advanced synthetic strategies in enhancing process efficiency. These agents predominantly share an N-(pyridin-2-yl)-pyri- midin-2-amine core scaffold, with their synthesis primarily dependent on metal-catalyzed cross-coupling reactions for C—N bond formation and condensation reactions for pyrimidine ring construction. Key challenges remain, including difficulties in regioselectivity control, significant reliance on precious metal catalysts, and limited scalability of current processes. Consequently, the development of greener, more cost-effective, and efficient synthetic methodologies represents a critical direction for future optimization in this domain.

The “carbonyl” functional group of the products in carbonylation reactions usually comes from gas carbon monoxide (CO) or its surrogates. Although gas CO as carbonyl source has wider substrate scope and can achieve industrial production, it is toxic and flammable. CO surrogates have stable chemical properties, which are easy to obtain. The reaction process is easy to operate and the separation/post-treatment is simple. Therefore, CO surrogates provide a variety of powerful and promising tools for the carbonylative conversion and construction of diverse chemicals. This review summarizes and discusses the latest progress in synthesizing high value-added chemicals using CO surrogates (carbon dioxide, chloroform, carboxylic acids and their derivatives, carbonyl metal reagents, acyl chlorides, etc.) as carbonyl sources. Finally, the development prospects and existing difficulties of different carbonyl sources in carbonylation reactions were discussed, in order to provide reference for promoting the development of more novel CO surrogates.

Cyclopentenone compounds are widely present in natural products and biologically active molecules, and act as very powerful synthons for the synthesis of a variety of bioactive target molecules. Therefore, it is of great research significance and application value to develop their synthetic methods. This article reports a novel method for the efficient synthesis of cyclopentenones by organic base-promoted [2+3] annulation reaction of arylglyoxal monohydrates with allyl phosphonium salts. This method displays metal-free, good chemoselectivity, mild reaction conditions, broad substrate scope, and short reaction time. The practical application of this method is demonstrated by the gram-scale synthesis and further transformation reactions.

2-Oxindole is a widely present skeletal structure in natural active products and drug molecules, and the radical cascade cyclization of N-arylacrylamide is the most effective method for synthesizing such compounds. Suitable free radical precursors can generate corresponding free radicals under the drive of light, electricity, or heat, thereby inducing a free radical cascade cyclization reaction of N-arylacrylamide to synthesize 2-oxindoles. Herein the research progress on the generation of free radicals induced by light, electricity, and heat in recent years and their application in the cascade cyclization of N-arylacrylamide to synthesize 2-oxindoles are systematically introduced.

Aliphatic amines are pivotal organic molecules, and therefore the precise C—H transformation of amines at distinct sites has long been a research focus in organic synthesis. Hydrogen atom transfer (HAT), recognized as a mild and controllable strategy for C—H activation, has attracted considerable attention in recent years and is extensively employed for the selective C—H transformation of amine molecules. By leveraging intermolecular or intramolecular HAT processes, it becomes feasible to precisely abstract C—H bonds at specific sites within amine molecules and facilitate subsequent transformations, providing novel synthetic pathways for the efficient construction of complex functional amine molecules. The recent advances in the selective functionalization of C—H bonds of amine molecules using the aforementioned strategy are comprehensively summarized. A review is conducted on the regio-, chemo-, and stereoselective regulatory mechanisms, as well as the reaction mechanisms involved. In addition, the limitation in this research field is analyzed and the outlook of this area is also prospected.

Polydopamine (PDA), as a “mussel-inspired” biomimetic material, has great application potential in the field of catalysis because of its non-toxic, environmentally friendly, stable and recyclable advantages. PDA contains a large number of catechol structures, which can reduce noble metal ions. Its widespread o-diphenol/o-quinone structure can also coordinate with cheap metal ions. Therefore, PDA can support metal to form heterogeneous catalysts. Meanwhile, the phenolic hydroxyl groups and amino groups contained in the PDA structure have acidic and basic effects, and they can also be used as catalysts. The application of M@PDA and PDA in a variety of organic transformations is reviewed, describing the catalytic efficiency and the number of cycles of the catalysts in detail. Moreover, the problems and challenges in this field are pointed out, which is expected to provide useful guidance for the future development of polydopamine materials in the field of heterogeneous catalysis.

As three-dimensional analogs of benzene, carboranes have attracted much attention in recent years in modulating the photophysical properties of organic chromophores and constructing organic luminescent compounds due to their unique three-dimensional cage geometries and electronic properties, in particular showing a unique role in the design and synthesis of aggregation-induced emission (AIE) compounds. In this review, the structural types and synthetic methods of carborane AIE compounds are summarized, with a special focus on the new advances in related synthetic methods. The main synthetic methods include constructing the o-carborane skeleton with suitable alkynes and decaborane (derivatives), reactions of aryl/alkenyl/alkynyl reagents with carborane derivatives, reactions of AIE species with carborane derivatives, transformation of carborane AIE compounds, catalytic B—H activation of carborane compounds, and deboronation of the closo-carborane cluster. Based on such progress, the research trends and application prospects of carborane AIE compounds are envisioned.

Optically active α,β-unsaturated γ-lactone and γ-lactam serve as core scaffolds in numerous natural products. These natural products exhibit a broad spectrum of bioactivities, making them highly significant for the development of novel drugs. Furthermore, as an important class of chiral building blocks, optically active α,β-unsaturated γ-lactone and γ-lactam play a pivotal role in synthesizing diverse bioactive compounds and complex molecules. Given their versatile biological activities and potential for structural diversification, the construction of such frameworks via asymmetric catalytic synthesis has received much attention from the academic community. This review summarizes the recent advances in asymmetric catalytic methods for synthesizing α,β-unsaturated γ-lactone and γ-lactam employing transition metal catalyst, Lewis acid catalyst and organo- catalyst, and discusses the stereocontrol mechanism in representative examples and the related application value.

Discovering new antibiotic drugs is a critical approach to addressing the issue of bacterial and fungal resistance. Developing novel antibiotic based on existing ones has proven to be an effective strategy. Currently, due to issues such as resistance and toxicity, many antibiotics have been developed into semi-synthetic drugs that are either on the market or in clinical trials. The complexity and stability of natural antibiotic products make the pharmaceutical chemistry development of semi-synthetic antibiotics particularly challenging, with subsequent synthetic processes presenting even greater difficulties. These process chemistries must address challenges in chemical, regio-, and stereo-selective transformations, as well as overcome technical obstacles in separation and purification. Over the century-long history of antibiotic development, chemists have developed many classic antibiotic chemical synthesis processes, such as tetracycline chemistry and macrolide chemistry. These classic semi-synthetic antibiotic processes are reviewed, detailing the chemical synthesis challenges, original and improved processes, and potential process optimizations.

Tuberculosis remains a significant global public health concern, particularly due to the increasing prevalence of drug-resistant tuberculosis, which poses substantial challenges to traditional treatment strategies. Bedaquiline, a novel class of anti-tuberculosis drug, offers a critical alternative for managing drug-resistant tuberculosis. However, the synthesis of this compound is one of the greatest challenges in synthetic chemistry due to its contiguous tertiary and tetrasubstituted chiral centers, necessitating advanced synthetic methodologies. Consequently, the advancement of efficient and environmentally sustainable asymmetric synthesis technologies has emerged as a key research priority. This review summarizes the synthetic pathways of bedaquiline, with an emphasis on pivotal technological approaches such as bimetallic catalysis. Furthermore, continuous flow technology, owing to its inherent advantages of efficiency, safety, and scalability, demonstrates considerable promise in the production of bedaquiline. Looking ahead, the integration of innovative catalytic systems, green chemistry principles, and intelligent manufacturing technologies will likely drive the evolution of bedaquiline synthesis toward greater efficiency and environmental compatibility, thereby facilitating large-scale production of anti-tuberculosis medications.

Chiral alcohol derivatives are an important class of molecules that exist in many bioactive substances and natural products, and are also an important class of organic synthetic intermediates used to synthesize many important organic compounds. Biomimetic catalysis has been emerging as a very powerful tool for catalytic asymmetric hydroxylation after biocatalysis, and this type of reaction is mainly innovative in the design of novel ligands and their application in asymmetric catalytic reactions. Therefore, it is of great significance to develop efficient, green and stereoselective methods for the synthesis of chiral alcohols. In this paper, the asymmetric hydroxylation of C—H bonds over the past two decades is summarized, and such reactions are classified and summarized according to the types of catalysts, which are mainly divided into two categories of biocatalysis and biomimetic catalysis.

Decarboxylation functionalization reactions of carboxylic acids via photocatalysis have garnered significant attention recently due to their operational simplicity and mild reaction conditions. Among these, photocatalytic decar- boxylation reactions based on transition metal complexes, particularly those involving ligand-to-metal charge transfer, represent an effective strategy. Due to the natural abundance and low toxicity of the iron element, photocatalytic decar- boxylation reactions involving iron complexes have gained huge attention. This review summarizes the recent advances in the field of light-induced iron-catalyzed decarboxylation functionalization reactions over the past two years, aiming to establish a foundation for the development of new methodologies.

Organosulfur compounds are widely found in organisms, natural products, biologically active molecules and functional materials, which also represent indispensable precursors and intermediates in organic synthesis. Based on the importance of these compounds, the synthesis of organosulfur compounds is one of the intriguing research topic. The cross-coupling reaction of C—S bonds under electrochemical conditions can construct inter- or intramolecular C—S bonds selectively, which provides an efficient, green and economical synthetic pathway for constructing organosulfur compounds with diverse structures. The progress of electrochemical C—S bond formation in recent years is discussed, classified by different functional groups of organosulfur compounds. The reaction mechanism and applicability are summarised, and the challenges and opportunities in this field are also prospected and discussed.

Nitroarene is one of the cheapest and most readily available raw materials in the chemical industry and is often used as multifunctional building blocks. In the past, the synthesis of nitrogen-containing compounds mainly depended on aniline. However, the utilization of nitroarenes can save one or more steps as compared to anilines. Therefore, the construction of nitrogen-containing compounds using nitroarenes as potential amino sources has become one of the research hotspots in recent years. Due to the advantages of radicals, such as high activity, mild reaction conditions, and good functional group compatibility, good progress has been made on radical-mediated activation of nitroarenes in recent years, and a variety of reaction types have been implemented. In this review, the recent progress in radical-mediated activation of nitroarenes under different catalytic conditions is summarized. The reaction substrate compatibility, mechanism, applications, advantages, and limitations in this field are also discussed in detail.

Phosphorothioates are a class of organophosphates containing S—P(O) bonds, which have important chemical and biological properties and are widely used in various fields such as organic synthesis, medicinal chemistry and agricultural chemistry. Therefore, the development of efficient and convenient methods for the preparation of phosphorothioates and their derivatives is of great significance in the research of phosphorus chemistry. In recent years, with the requirements of sustainable chemical development, photocatalysis and electrocatalysis as green and friendly strategies have attracted wide attention from chemists. This review introduces the research progress of photosynthesis of phosphorothioates, including metal-free photocatalysis, metal photocatalysis, dye photocatalysis, photoredox and metal co-catalysis, and electrooxidation reactions without external metals and catalysts.

A chromium(II)-catalyzed reduction cross coupling reaction was reported. This reaction utilizes inexpensive and readily available chromium dichloride as a catalyst and 4,4'-di-tert-butyl-bipyridine as a ligand to achieve reduction cross coupling between trifluoromethyl olefins and alkyl bromides under mild conditions, effectively synthesizing difluoroalkene derivatives. This reaction exhibits good substrate universality and is compatible with multiple important functional groups, providing a concise synthetic pathway for constructing conjugated difluoroalkenes containing allyl difluoromethylene structural units. Preliminary mechanistic experiments indicate that alkyl bromides first undergo a reduction process to generate corresponding alkyl radicals, followed by addition to trifluoromethyl olefins. After binding with Cr(II), they undergo a β- fluorine elimination process to generate difluoroalkenes.

An efficient and practical synthetic process for Daprodustat was developed. Starting with N,N'-dicyclohexylcarbo- diimide (DCC) and malonic acid, the key intermediate 1,3-dicyclohexylpyrimidine-2,4,6(1H,3H,5H)-trione was synthesized via condensation reaction with 91% yield. Subsequent activation of this intermediate by 1,1'-carbonyldiimidazole (CDI), followed by a one-pot reaction with glycine ethyl ester hydrochloride, directly afforded Daprodustat in 92% yield with >99.8% HPLC purity. The process achieved an overall yield of 84% upon validation at 62-gram scale. Structural confirmation of the key intermediate was accomplished through nuclear magnetic resonance (NMR) spectroscopy and high-resolution mass spectrometry (HRMS). Compared with existing methods, this streamlined protocol demonstrates advantages including simplified operation, reduced reaction time, and lower production costs, offering significant potential for industrial-scale synthesis of Daprodustat.

Synthesis methods of quinoline and isoquinoline rings have gradually occupied an important position in the field of medicine and chemical industry. Their special heterocyclic structures make them important lead compounds in medicinal chemistry and organic chemistry. Quinoline and isoquinoline molecules have anti-malaria, anti-Alzheimer’s disease, anti-tumor, anti-hypertension, anti-oxidation, antibacterial and other biological activities. The significance of quinoline and isoquinoline derivatives in the field of medicinal chemistry and organic chemistry is reviewed, and then the research progress of new and improved traditional synthesis methods, including transition metal catalysis, photocatalysis and microwave catalysis under the condition of metal and non-metal catalysis, in recent years is systematically reviewed, so as to obtain different substituted or cyclized quinoline or isoquinoline compounds.

Catalytic technology holds irreplaceable significance in modern science and industry, and has played a crucial role in biomedicine, green chemistry, and other fields. Macrocycles, with their unique ability for molecular recognition and the formation of inclusion complexes through non-covalent interactions, exhibit highly efficient catalytic performance. Among them, chiral macrocycles, leveraging their chiral characteristics, can achieve efficient chiral induction and selective recognition. Their internal cavities can accommodate substrates for pre-organized arrangement, thereby facilitating efficient chemical transformations. Therefore, chiral macrocycles serve as an ideal platform for supramolecular catalytic systems, demonstrating excellent catalytic activity and selectivity in asymmetric catalysis. This review summarizes the research progress and applications of chiral macrocycles, such as chiral crown ethers, chiral cyclodextrins, chiral calixarenes, and chiral pillararenes, in asymmetric catalysis in recent years, and is expected to provide references for the study of supramolecular asymmetric catalysis.

The development of sterically hindered aryl-alkyl coupling reactions is of great significance in promoting the advancement of organic synthesis and electronic materials. A conformationally well-defined, sterically hindered, electron-rich monophosphorus ligand ^PAd-AntPhos was designed and synthesized, and its application as a ligand in the palladium-catalyzed Suzuki-Miyaura coupling reaction between sterically hindered aryl halides and cyclic alkylboronic acids were studied. To develop an efficient sterically hindered aryl-alkyl coupling reaction, a more sterically hindered ^PAd-AntPhos based on the structure of AntPhos was designed and synthesized. In the coupling reaction between 2,4,6-triisopropyl bromobenzene and cyclohexylboronic acid, ^PAd-AntPhos has shown excellent reactivity, yielding the target product in 80% yield by screening various reaction conditions including ligands, temperature, and bases. A series of sterically hindered aryl-alkyl coupling products have been obtained in unprecedentedly high yields. Compared to AntPhos, ^PAd-AntPhos has shown good tolerance of steric hindrance.

Cyclohexene is an easily available chemical raw material that can be prepared by selective hydrogenation of benzene. Compared with cyclohexane, the introduction of the alkene functional group makes cyclohexene more active and can be oxidized with better selectivity. Therefore, the oxidation reaction of cyclohexene is the key step for the synthesis of nylon-66 series products and their intermediates. In recent years, selenium catalysis technology has developed rapidly. Compared with metal catalysis, selenium is easily metabolized and ecologically safe, and its catalytic oxidation process usually uses hydrogen peroxide and molecular oxygen as clean oxidants, which are environmentally friendly. The selenium-catalyzed oxidation technology of cyclohexene is expected to be applied in the synthesis of nylon intermediates. The relevant progresses including both homogeneous and heterogeneous catalysis are reviewed, the principle from a scientific perspective is expounded and prospects for its industrial application are provided.

Morphine alkaloids have long been regarded as one of the core challenges in synthetic chemistry due to their complex polycyclic skeletons and significant pharmacological activities. The research progress in the total synthesis of morphine alkaloids reported from 2017~2024 is summarized, with a focus on analyzing innovative synthetic strategies aimed at precisely constructing core polycyclic skeletons and key chiral centers. These studies not only demonstrate the science and art of synthetic chemistry, but also lay an important foundation for promoting the industrial production of morphine alkaloid drugs and the development of new pharmaceuticals.

Helicenes and their derivatives represent a class of non-planar nanocarbon molecules formed by ortho-fused aromatic rings. Their unique helical structure endows helicenes with remarkable chiral optical activity, exhibiting circular dichroism (CD) and circularly polarized luminescence (CPL) properties. These characteristics make helicenes highly promising for applications in optical materials and biosensors. Heteroatom doping is an effective strategy to enhance the performance of helicenes. By introducing heteroatoms such as nitrogen, boron, oxygen, or sulfur, the electronic structure of helicenes can be precisely tuned, significantly improving their chiral optical properties and quantum yield. The latest research progress in this field over the past three years is summarized, focusing on the design, synthesis, and performance optimization strategies of all-carbon helicenes and heteroatom-doped helicene nano-carbon molecules. Future development directions are also discussed.

Ketones, as precursors to dihydroquinazolinone derivatives, are a class of commercially available bulk chemicals and serve as an active scaffold that is widely present in nature. In recent years, dihydroquinazolinone compounds synthesized from ketones as starting materials have proven to be excellent reagents for organic functionalization, with related studies being reported consecutively. These reagents can generate reactive radical intermediates via single-electron transfer (SET) and C—C bond cleavage, subsequently undergoing various chemical transformations to build important organic molecules. This article provides an overview of the recent advancements in free radical reactions involving dihydroquinazolinone compounds derived from ketones, discussing topics such as reaction design, mechanisms, and future research prospects. This article provides an overview of the recent advancements in free radical reactions involving dihydroquinazolinone compounds derived from ketones, discussing topics such as reaction design, mechanisms, and future research prospects.

Aggregation-induced emission (AIE) photosensitizers have emerged as a new generation of candidates for photodynamic therapy (PDT) owing to their ability to maintain strong fluorescence and efficiently generate reactive oxygen species (ROS) in polymerized and aggregated states. Focusing on the recent research progress in molecular electronic structure and molecular motion regulation strategies, synthetic methodologies for constructing donor-acceptor (D-A) frameworks (such as Suzuki-Miyaura coupling, Stille coupling, Buchwald-Hartwig coupling, Sonogashira coupling, and Knoevenagel condensation), strategies for tuning π-conjugated backbones (such as the Heck reaction and Vilsmeier-Haack reaction), methods for enhancing spin-orbit coupling (SOC) including Menshutkin reactions, click chemistry, and metal coordination reaction, as well as motion-restricting strategies, including polymer encapsulation and nanoparticle loading, are mainly summarized. Through synergistic multidimensional molecular design and materials engineering, AIE photosensitizers have achieved significant improvements in near-infrared imaging and deep-tissue PDT efficacy. Looking forward, machine learning-assisted molecular screening and multimodal delivery platforms accelerate their clinical translation toward precision phototherapy of deep solid tumors.

Recent studies have demonstrated that 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (Binap) based bisphosphonium salts Binap(OTf)₂ exhibit excellent catalytic performance in visible light photoredox catalysis, holding promise as a competitive class of visible-light catalysts. Binap(OTf)₂ was successfully utilized to catalyze the cyclization of aryl alkynes with N-imine(iso)quinoline ylides under blue light, addressing the limitations of substrate availability or accessibility in the current synthesis of β-aryl-substituted pyrazolo(iso)quinoline compounds. This approach provides a new strategy for the construction of pyrazolo(iso)quinoline compounds.

Diaryliodonium salts, which serve as highly electrophilic arylation reagents, have been widely used in organic synthetic chemistry due to their environmental compatibility, remarkable stability, and excellent selectivity. As novel reagents, they can produce aryl radicals to synthesize aromatic compounds. The research progress achieved in the past decade regarding the construction of carbon-carbon and carbon-heteroatom bonds by utilizing aryl radicals derived from diaryliodonium salts is summarized with content mainly divided into two parts: arylation induced by visible light and arylation without photocatalysis. Their applications in the synthesis of bioactive arylated heterocyclic compounds are also discussed.

Carbazolequinone natural products have attracted extensive attention due to their good antimalarial, antitumor, and antiviral biological activities, making them a prominent research target in the field of medicinal chemistry. The synthesis strategies of carbazolequinone compounds are summarized in the past three decades, mainly including transition metal catalysis (palladium, copper, ruthenium, etc.), transition metal-free catalysis and oxidation reaction methods, which can be used to synthesize carbazolequinone compounds in a concise and efficient manner. Moreover, future research directions are envisioned, including the development of more efficient catalytic systems, expansion of substrate scope and advancement of green synthesis methods. These efforts aim to broaden the application prospects of carbazolequinone compounds in drug development. Finally, an in-depth exploration of their structure-activity relationships provides novel strategies and insights for the discovery and design of new drugs based on the carbazolequinone scaffold.

A Silver-catalyzed enantioselective [3＋2] cycloaddition of azomethine ylides with activated alkenes by using a P-stereogenic ligand Ganphos is reported. The method provides an efficient strategy for the effective synthesis of spirocyclic scaffolds containing a pyrroline motif. Notable features of this approach include good yields, remarkable enantioselectivity, as well as a broad substrate scope and significant step efficiency.

As naturally abundant and readily available starting materials, alcohols are frequently employed as synthetic building blocks in organic synthesis. The hydroxyl group, which serves as the characteristic functional group of alcohols, is the primary reactive site for these compounds. Consequently, dehydroxylative functionalization reaction is one of the representative transformations of alcohols and has demonstrated significant potential in constructing new chemical bonds. Over the past decade, this research field has received continuous and extensive attention. This review comprehensively summarizes the recent advances in the dehydroxylative functionalization of alcohols, discussing on the reaction methodologies and mechanisms for constructing carbon-heteroatom and carbon-carbon bonds from alcohols.

Molecular oxygen is regarded as an ideal oxidant due to its abundant content, low cost and non-polluting nature. However, reactions involving dioxygen at room temperature usually suffer from slow rates and low selectivity, and thus require the assistance of enzymes, metal catalysts or other conditions to promote transformation. Visible light-induced organic reactions have attracted extensive attention from chemical researchers due to their simple operation steps, green and sustainable nature as well as mild reaction conditions. In recent years, visible light-induced oxidation difunctionalizations of olefins with molecular oxygen have witnessed swift advancement and became one of the research hotspots in the field of organic synthesis. The recent research progress in the synthesis of oxygen-containing compounds through visible light-catalyzed oxidative difunctionalizations of alkenes with dioxygen is summarized. The selected examples of substrates and the corresponding reaction mechanisms are described, and the development of this field are also prospected.

1,3-Enynes are a class of organic molecules with both alkyl and alkenyl groups, which have unique structural properties and have been used as the basic units in a variety of reactions to obtain a variety of specialized molecular structures. Selective difunctionalization of 1,3-enynes is an attractive strategy for the construction of 1,3-diene-type compounds, alkyne-based compounds, aromatic heterocycles such as thiophenes and pyrroles, as well as multisubstituted allene derivatives. In recent years, various catalytic strategies for the difunctionalization of 1,3-enynes have been widely reported, however, challenges in controlling the chemo- and regioselective difunctionalization of 1,3-enynes persist. The 1,2-, 3,4-, and 1,4-difunctionalization reactions of 1,3-enynes in the last few years are summarized, and the directions of development in this field are prospected.

A dearomatization strategy using dicetolic acid (6) as the starting material to synthesize the core intermediate (10R,13S,14S)-10,13-dimethyl-7,10,11,12,13,14,15,16-octahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione (20) for the formal synthesis of dydrogesterone is presented, achieving a total yield of 21% over nine steps. This approach features an environmentally friendly carbonyl protection strategy and efficient Heck coupling, while avoiding harsh conditions and hazardous reagents throughout the entire process.

A series of potentially bioactive indolones were synthesized under light irradiation via catalyst-free electron donor-acceptor (EDA) complexes formed between arylthionium salts and unsaturated arylamide compounds. The photoexcited EDA complex generated an aryl radical, which subsequently underwent radical addition followed by intramolecular cyclization to yield the desired products. The reaction exhibited high regioselectivity. Additionally, based on preliminary studies of the reaction mechanism, a plausible catalytic cycle for the tandem radical reaction has been proposed.

Entecavir is a carbocyclic analogue of 2'-deoxyguanosine developed by Bristol-Myers Squibb (USA) in 1997 with potent and selective activity against the hepatitis B virus (HBV). Its structure consists of a five-membered ring and a guanine moiety. Clinically, it demonstrates strong inhibitory effects against the hepatitis B virus and has a relatively low tendency for drug resistance. This review provides a comprehensive summary of reported total and formal syntheses of entecavir to date, covering both early classical strategies and more recent asymmetric approaches featuring high selectivity and efficiency. It emphasizes the key reaction steps in various synthetic pathways. These synthetic efforts not only advance the process development of entecavir but also offer valuable insights for the synthesis of structurally related nucleoside-based antiviral agents.

Efficient construction of complex and high value organic molecules from simple and readily available starting materials is a core objetive of organic synhthesis. In recent years, transition metal-catalyzed C—H bond activation, facilitated by directing groups, has been demonstrated as a powerful strategy for achieving site-selective functionalization. Among various substrates, arylcarboxylic acids have gained significant attention as ideal starting materials due to their structural diversity, high stability, and easy accessibility. Notably, the carboxyl group can serve as a traceless directing group, eliminating the need for additional directing group installation and removal steps, thereby significantly enhancing atomic and step economy. Benefiting from these advantages, transition metal-catalyzed decarboxylative C—H bond mono-functionalization of aryl carboxylic acids has achieved remarkable progress. However, the development of difunctionalization remains underdeveloped, despite its significant synthetic value and application potential in rapidly constructing complex organic structures. This review summarizes the recent advances in traceless carboxyl-directed C—H monofunctionalization and difunctionalization, and discusses the challenges and future directions in this field.

A metal-free, visible-light-induced strategy has been developed for the diborylation of gem-dibromoalkanes. This reaction enables the construction of structurally diverse alkyl gem-diboronates at room temperature via visible-light-induced C—Br bond activation using B₂cat₂ as the boron source. Through a tandem in-situ dibromination/diborylation process, a one- pot transformation from aldehydes to alkyl gem-diboronates has been achieved. Additionally, sunlight irradiation has been demonstrated as a viable alternative for inducing this reaction, enabling gram-scale synthesis with practical applicability.

Organic-inorganic hybrid clusters with strong X-ray radioluminescence have exhibited great potential in scintillator field. However, fabricating the X-ray imaging screens of the clusters without sacrificing the scintillation performance is challenging. Herein, we report an effective way to prepare high-quality scintillation films of two synthesized Cu(I) clusters through vacuum evaporation deposition. The developed Cu(I) clusters with rigid molecular structures show excellent scintillation performance with a high light yield of up to 19356.7 photons/MeV and a low detection limit of 158 nGy/s. The scintillation film based on the Cu(I) clusters made by vacuum evaporation deposition is highly uniform with a small surface roughness value of 1.04 nm, which can be applied to X-ray imaging for various objects. These results not only provide important guidance to develop high-performance organic-inorganic hybrid scintillators, but also pave a straightforward way to prepare non-doped scintillation screens for remarkable X-ray imaging applications.