The spirooxindoles have broad and promising activities in various therapeutic areas, and become a privileged skeleton for drug discovery. Therefore, the development of some simple and efficient strategies to build these sophisticated scaffolds has become one of the most widespread concerns. However, the traditional methods are limited by the separation and purification of intermediates, the functional group protection and de-protection. Recently, the cascade strategies have shown special advantages in the synthesis of optically active natural products and complex molecules, many related studies have been reported. This review summarizes the enantioselective synthesis of spirooxindoles via cascade strategies in the past five years and organized on the basis of four types of starting materials: unsaturated oxindole derivatives, C(3)-substituted oxindoles, C(3)-unsubstituted oxindoles and nonoxindoles.

The recent advances in the synthesis of organic pyrophosphate are reviewed, based on the coupling methods including dicyclohexylcarbodiimide (DCC), N,N'-carbonyldiimidazole (CDI), DCC/morpholine/MnCl₂/MgSO₄, DCC/ morpholine/1H-tetrazole, PPh₃/(PyS)₂/N-methylimidazole, diphenyl phosphorochloridate (DPCP), trifluoroacetic anhydride/N-methylimidazole. Mechanism of some reactions is also discussed.

Novel N-benzoyl-N'-phenylthioureas containing imidazolidine-2,4-dione were prepared from substituted benzoyl chlorides via isothiocyanate formation followed by treatment with 5-(4-aminophenyl/benzyl)imidazolidine-2,4-dione. The base-catalyzed condensation of thioureas with bromoacetone was carried out in the presence of triethylamine to afford the corresponding 4-methyl-3-substituted-phenyl-2-acylimine thiazolines in moderate to good yields. The corresponding thiazolines were characterized by IR, ¹H NMR, HR-ESI-MS spectroscopic data and X-ray diffraction analyses, and the mechanism of thiourea reacting with bromoacetone was re-confirmed by the X-ray structures of compounds 3g and 4g. The thiazolines were evaluated their biological activities, and some of them exhibited significant activities such as compounds 3i and 4q having 82.6% and 100% mortality against P. xylostella at the concentration of 200 mg/L, 4n having 82.6% inhibitory rate against S. scleotiorum at 50 μg/mL, and slight but not significant herbicidal activities.

The background, principle and sorts of organic solar cell have been reviewed. The organic solar cell materials are presented in detail, which includes small molecule solar cell material, macromolecule solar cell material, D-A material and inorganic/organic hybrid material.

Mitsunobu reaction is one of the most efficient methods for the construction of the C—O, C—N, C—S and C—C bonds under mild and neutral conditions which is widely used in the total synthesis of various natural products and the transformation of functional group, and this paper reviews the recent progress of such reaction.

The determination of the absolute configuration (AC) of chiral molecules is an important issue in organic chemistry. Vibrational circular dichroism (VCD) is a useful technology to measure the circular dichroism of chiral molecules in the IR region, which remarkably expands the application of circular dichroism to the determination of AC. The AC of chiral molecules can be determined by comparison of the experimental VCD spectra with the theoretical VCD ones obtained on the basis of quantum chemical calculations.

This paper reviews the recent progress of all kinds of reductive amination methods and their applications in organic synthesis, particularly emphasis on the introduction to the reductive amination with high efficiency and high selectivity.

The current review presents the advances in PEGylation of drug conjugates based on plentiful literatures up to date. The physiochemical properties of PEG [poly(ethylene glycol)] and advantages of PEGylation for drug conjugates are introduced briefly. The technology of PEGylation of protein and small molecular drug conjugates and application to drug investigation are presented in detail. It is found that PEGylation technology can effectively improve the pharmacokinetic and pharmacodynamic properties of drugs by altering the structures of drug conjugates. It also presents a method to extend the area of clinic application of drug conjugates. The foresight of development and investigation of PEGylation of drug conjugates is also brought forward based on the discussion of advantages and investigation status in quo of PEGylation tech-nology.

This paper reviews the applications of 2-iodoxybenzoic acid (IBX) in organic synthesis, focusing on the oxidations of IBX with alcohols, nitrogen-containing, sulfur-containing organic compounds, selective oxidation at carbon adjacent to aromatic systems, preparations of α,β-unsaturated carbonyl compounds and lactones, etc. These reactions take place in mild conditions, in high yields, and with high chemoselecticity. IBX-amide, IBX-ester and polymer-supported IBX analogues, which are mild, non-explosive, highly soluble, and/or recyclable, are also discussed.

The method of reduction of 2,2',4'-trichloroacetophenone with sodium borohydride to prepare 1-(2,4-dichlorophenyl)-2-chloroethanol was studied. Temperature effect on the reaction was investigated and the mechanism to form objective product and byproducts was discussed. Calcium chloride and lanthanum chloride etc. efficiently improved the reaction specificity. In the presence of amberlyst-732(H^＋) the reaction was smoothly carried out in aprotic solvent such as THF with high yield and specificity. The structure of the objective product was characterized by IR, ¹H NMR and ¹³C NMR spectra.

In this review, discovery, history, reaction mechanism, reaction scope and limitation of Huang-Minlon reduction are described.

Nickel-catalyzed C—C and C-heteroatom cross-coupling reactions are reviewed. The reactions include Heck reaction, Sonogashira reaction, Kumada-Corriu reaction, Negishi reaction, Stille reaction, Suzuki reaction, Ullmann reaction, C—N coupling, C—O coupling, C—P coupling, and C—S coupling. The substrates, reaction conditions, selectivities and yields of these reactions are described. The mechanistic studies on Ni-catalyzed reactions were also surveyed.

The very recent progress in Sonogashira reactions is summarized, which includes the optimization of the reaction conditions, tandem Sonogashira reactions, green Sonogashira reactions, and non-Pd Sonogashira reactions. The mechanistic studies on Sonogashira reactions are also surveyed.

Fluoro-substituted phenylboronic acids are very important organic synthesis intermediates, which have been widely used in organic synthesis. A progress in the preparation and application of fluorosubstituted phenylboronic acids is reviewed.

The recent advances in the selective monoprotection of diols are reviwed. The monoprotection of diols could be realized by a lot of organic reactions, such as monoetherification and monoesterification of diols. The development of monoprotection of diols by the chiral reagents and bio-catalysts and the application of monoprotection of diols in the synthesis of natural products are also discussed.

Organocatalytic asymmetric reaction is an increasingly active area in organic synthesis. The asymmetric Michael addition provides a rapid access to versatile important chiral building blocks and intermediates for the synthesis of bioactive agrochemicals and pharmaceutical compounds. The reported organocatalyst for asymmetric Michael additions include proline and its derivatives, chiral imidazolidinone derivatives, chiral (thio) urea, cinchona alkaloids and so on. The applications of various organocatalysts to asymmetric Michael additions are reviewed in this paper. The reaction mechanism, catalytic activity and the asymmetric induction influenced by the structure of organocatalysts and the reaction condition are also discussed.

Fluorination is widely used in organic synthesis. As a kind of fluorinating reagent, triethylamine tris(hydrofluoride) has the advantage on top of others. Several applications of triethylamine tris(hydrofluoride) to organic synthesis are summarized according to reaction type, especially for nucleophilic substitution, the ring-opening fluorination reaction of epoxide, electrophilic addition, desilylation reaction and so on.

mTOR, a serine/threonine kinase, is a target molecule of rapamycin. In cells, mTOR acts as the catalytic subunit of two functionally distinct complexes, called mTORC1 and mTORC2. These complexes coordinate a variety of processes that include gene transcription, protein translation initiation, ribosome biosynthesis, apoptosis and many other biological processes. Dysregulation of mTOR signal pathway is closely related with tumorigenesis. Inhibition of mTOR pathway leads to an effective block of abnormal signal transduction and blocks the development of cancer. Traditional mTOR inhibitors are rapamycin and its derivatives, among which everolimus and temsirolimus have already been approved for the treatment of renal-cell carcinoma. In addition, a number of small molecule inhibitors of mTOR, including several PI3K/mTOR dual inhibitors, have been developed. NVP-BEZ235, PKI587, PKI179, GSK2126458, AZD8055 and WYE-354 have entered the clinical stage.

Pd(II)-catalyzed reactions were developed using β-heteroatom elimination and protonolysis reaction to quench the carbon-palladium bond in the presence of halide ions or nitrogen ligands (pyridine, bipyridine, phenanthroline, etc.) for the regeneration of the divalent palladium species. Halide ions or nitrogen ligands are necessary for the catalytic cycle and high yield of the reactions. For Pd(0)-catalyzed reactions, control of β-hydride elimination is also a challenge for making coupling reactions more diversified. Different kinds of ligands were used to make the coupling reaction suitable for aliphatic compounds. Recently, examples using chloride ion or bathophenanthroline for this purpose were also developed.

Flavonoids are a kind of secondary metabolite of plants, which are widely distributed in almost all plants owing to huge diversity in the category and configuration. Flavonoids, with unique chemical structures, are bearing many important physiological and biochemical effects on mammals and other types of cells. Adequate intakes of flavonoids are reported to be associated with reduced risks of cancer, tumor, car-diovascular disease, lipid peroxidation and osteoporosis. With increasing research of the structure-activity relationship, functionary mechanism of partial pharmacological actions is discovered. This progress provides a theoretical basis of flavonoids for their application to medicine and food industry, and certainly accelerates their development. In this essay, the physiological activities and research advance in synthesis of flavonoids are summarized.

This paper reviewed the advances of aryl-aryl coupling reactions in the past several years, including the feature, mechanism and application of different aryl-aryl coupling reactions. Particularly, the stereo- and regio-selective coupling methods were described.

Thioureas can be used in various areas．Based on different starting materials, reagents, solvent and catalysts, the recent ten-year progresses in the synthetic methods of thioureas are reviewed emphatically．

Through the introduction of drug loading mechanism, drug controlled release mechanism, and targeting methods of mesoporous silica nanoparticles (MSN), the application of MSN to controlled drug delivery system is reviewed.

P450 enzymes are ubiquitous heme-containing monooxygenases and involved in a number of vital processes including carcinogenesis and drug metabolism as well as the biosynthesis of steroid hormones and fat-soluble vitamin metabolism and the conversion of polyunsaturated fatty acids to biologically active molecules. Recent advances in understanding structure-function relationships in cytochrome P450 are summarized. Of particular importance is the role that plays in P450 function, where the active site undergoes large open/close motions to enable substrates to bind and products to leave and electron transfer pathways.

Fluorinated compounds comprise a substantial proportion in the therapeutic drugs. It is an important strategy to introduce fluorine and fluorinated substitutes in the small molecule for structure-based medicinal chemistry. They can modulate the physicochemical and pharmacokinetic properties to improve bioavailability, alter the conformation of a molecule to enhance the selectivities and binding affinity to target proteins, and block metabolically labile sites to increase the metabolic stability of drugs.

Click chemistry has attracted great interests due to a wide variety of superior merits, including a wide range of applications, simplified experimental condition, rapid reaction speed, higher functional group conversion, environmental friendly and selectivity. And conception of click chemistry contributed to the synthetic chemistry apparently, in particular, with respect to pharmaceutical manufacture and biomedical materials, resulting in the most useful and promising synthetic method. Furthermore, thiol-ene/yne click chemistry, utilizing inclusion of visible light or UV light as catalytic medium, is a comparatively novel kind of click chemistry in comparison to several types of conventional reactions. In addition, the properties of the creative reaction stems from the combination the photoinitiated chemical reaction with the forementioned traditional click chemistry, providing a flexible approach to occur reaction within the oriented region and functional group. This review highlights the recent research on the preparation of functional polymeric microsphere, amphipathic block well-defined polymer, materials employed in the molecular device, desired dendritic polymers and chemistry modification via thiol-ene/yne click chemistry. Moreover, the problems and solutions are given for the future development of thiol-ene/yne click chemistry.

Carbazole and its derivatives are an important type of nitrogen-containing aromatic heterocyclic compounds, possess desirable electronic and charge-transport properties, as well as large π-conjugated system with rigid fused rings. These special structures of carbazole compounds endow their distinct various functions, properties and biological activities, as well as wide potential application in photoelectrical materials, dyes, medicinal agents, supramolecular recognition and so on. More importantly, the carbazole compounds are easily modified and various functional groups could be conveniently introduced into the carbazole ring. The syntheses of carbazole derivatives and their potential applications were extensively investigated and have been become highly active highlight in recent years, and the progress is quite rapid. Combining with our researches and referring other works from literatures, this paper systematically reviews the recent advance in the research and development of carbazoles in organic electro-luminescence materials, organic photorefractive materials, solar cells, dyes, medicinal chemistry, supramolecular recognition and so on. The perspectives of the foreseeable future are also presented.

This paper reviewed the recent advances of Glaser coupling reaction and its applications to the synthesis of conjugated polymers. The reaction mechanism was also discussed.

n this review, the basic concept of click chemistry, as a new synthetic method, is introduced with its applications to lead discovery, optimization, proteomics and DNA research in recent years.

For the Friedel-Crafts acylation, the kinetic studies, the structure discussion and properties of the intermediate have been summerized. Basing on these studies, the possible mechanisms have been proposed and explained. According to the foregone results, a lot of indistinct doubts remain exist and the direction for the development of the kinetic and mechanism is put forward.

Recent development of the palladium-catalyzed Stille cross-coupling reactions is reviewed, which includes (1) the reactions of organotin compounds with organic electrophilic reagents such as aromatic halides, alkyl halides, and acyl chlorides etc., (2) mechanisms of the palladium-catalyzed Stille reaction, and (3) the applications of the Stille reaction to organic synthesis.

The recent application of I₂ as an effective catalyst to organic synthesis was reviewed, mainly focusing on reactions of selective deprotection of ethers, esterification and transesterification, acetalization and ketalization, electrophilic substitution and aziridination of olefins.

The transition metal-catalyzed cross-coupling reaction to form sp2 C—C or C-hetero atom bonds is one of the most important methods for modern organic synthesis。In comparison with Pd and Ni，copper is a cheap metal with low-toxicity。In this review the newest development of the Cu catalysts in C—N cross-coupling reactions is summarized.

Recently visible light photoredox catalysis was widely used in organic synthesis. Due to its low cost, easy availability and environmental friendliness, it has become one of the fastest growing fields in organic chemistry. This review summarizes recent development and application of visible light photoredox catalysis in organic synthesis and also gave its outlook in the future.

The recent progress of calixarene derivatives chemistry was reviewed in some aspects: molecular recognition enzyme mimic chemical sensor molecular assembly optoelectronic and nano material. Especially a considerable attention was paid to studies in China.

Tailor-made α-amino acids have played an important role in current life science research and biomedical development. Among the methodologies of α-amino acid asymmetric synthesis, chiral auxiliary strategy received most intensive and extensive investigations. Recent development in this strategy was outlined. Detailed critical review on the glycine equivalent approach in the last ten years was given.

Protein tyrosine kinases (PTKs) play a pivotal role in the signal transduction pathways, and their deregulation is highly related with the oncology including bladder, breast, colon, and lung cancers. Com-pounds that inhibit the kinase activity of PTKs are potential chemotherapeutics to treat tumors. With the emergence of the multiple drug resistance of tumor cells against the existing PTK inhibitors, new mechanism PTK inhibitors are designed and developed. This review is focused on the recent advance of the discovery and development of the small molecular PTK inhibitors, categorized according to the mode of ac-tion. Furthermore, the synthesis of the typical structures is described.

Although oxa-Michael reaction is an important protocol and often applied in the total synthesis of natural products, it has only recently gained considerable interest. This review deals with the new development of oxa-Michael reaction.

Biphenyls is an important kind of organic synthesis intermediate. It can be synthesized by organometallic coupling reaction which is an impotrant method for constructing biphenyl bond. Methods of the synthesis of biphenyls are reviewed classified by reaction substrates. The cross-coupling of aryl metal compounds with aryl halides is introduced in detail.