Chinese Journal of Organic Chemistry 2025, 45(9)

- About the Cover:
  
  The recent advances in the synthesis of bedaquilinebased antitubercular agents are reviewed by Gao and Zhang on page 3113, with emphasis on key strategies such as bimetallic cooperative catalysis. Furthermore, continuous flow technology, owing to its inherent advantages of efficiency, safety, and scalability, demonstrates considerable promise in the production of bedaquiline. Bedaquiline-based drug synthesis will become more efficient, green, and sustainable.
- About the Cover:
  
  The fluorescence molecular design models based on various machine learning (ML) algorithms are reviewed by Guo, Li, Tang, and Fan on page 3203. The current research is categorized according to multiple diagnostic and therapeutic molecular characteristics, and the future development directions for molecular design using ML methods are proposed.
- About the Cover:
  
  A novel method for the efficient synthesis of cyclopentenones by organic base-promoted [2＋3] annulation of arylglyoxal monohydrates with allyl phosphonium salts has been successfully developed by Zhang, Jiang, Xin, Huang and Wang on page 3420. This method displays metal-free, good chemoselectivity, mild reaction conditions, broad substrate scope, and short reaction time.
- About the Cover:
  
  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 by Yao, Wang, Yuan, Zeng, Jiang, Zou, Ren, Zhang, and Zeng on page 3478, achieving a total yield of 21% over nine steps. This approach features an environmentally friendly carbonyl protection strategy and efficient Heck coupling.
2025, 45(9)

25 September 2025
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REVIEWS ARTICLES HIGHLIGHTS

REVIEWS

Advances in the Process Chemistry of Semisynthetic Antibiotics Based on Complex Natural Products^★

Hua-Nan Wang, He Wu, Ye Zhao, Yi Gu, Gang Chen

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3045-3074 DOI: 10.6023/cjoc202506002

Abstract( 283) HTML( 48) PDF(1095KB)( 154 )

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Applications of Precise Chemistry in Drug Discovery^★

Rong Liu, Yinglin Zuo, Yingjun Zhang, Ji Zhang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3075-3097 DOI: 10.6023/cjoc20205031

Abstract( 122) HTML( 10) PDF(1770KB)( 102 )

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Recent Progress in the Total Synthesis of Morphine Alkaloids^★

Xiaoyu Liu, Tingrui Xu, Yong Qin

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3098-3112 DOI: 10.6023/cjoc202505029

Abstract( 176) HTML( 19) PDF(832KB)( 174 )

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Advances in Bedaquiline-Based Antitubercular Drug Synthesis^★

Feng Gao, Wanbin Zhang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3113-3127 DOI: 10.6023/cjoc202505017

Abstract( 181) HTML( 21) PDF(2852KB)( 183 )

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Precise Synthesis of Proteins/Peptides: Advances in Single-Site Selective Chemical Modification and Automated Synthesis Technologies^★

Cheng Ren, Chengxi Li

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3128-3147 DOI: 10.6023/cjoc202505023

Abstract( 151) HTML( 10) PDF(2035KB)( 61 )

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Advances in Glycosylation Reactions Promoted by Trivalent Iodine Reagents^★

Yulin Tan, Zhihua Liang, Wei Chen, Lingkui Meng, Jing Zeng, Qian Wan

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3148-3162 DOI: 10.6023/cjoc202507032

Abstract( 104) HTML( 7) PDF(870KB)( 83 )

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Advances in Chiral Recognition and Asymmetric Catalysis of Minimal Structural Differences Compounds^★

LüYa, Guihan He, Jianjian Liu, Yongzheng Chen

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3163-3174 DOI: 10.6023/cjoc202506025

Abstract( 110) HTML( 9) PDF(805KB)( 71 )

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Advances in Understanding the Substrate Promiscuity of Alcohol Dehydrogenases/Carbonyl Reductases^★

Youxue Zhao, Xiruo Li, Luobing Meng, Chunxiu Li, Guisheng Fan, Jianhe Xu

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3175-3185 DOI: 10.6023/cjoc202506006

Abstract( 106) HTML( 6) PDF(8746KB)( 106 )

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Progress in Total Synthesis of Entecavir, an Antiviral Drug for Hepatitis B^★

Ying Xia, Chenlong Zhu, Bingfeng Sun

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3186-3202 DOI: 10.6023/cjoc202504011

Abstract( 148) HTML( 10) PDF(973KB)( 96 )

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Advances in Machine Learning-Based Design of Organic Fluorescent Theranostic Molecules^★

Haozhe Guo, Yuyin Li, Peichen Tang, Jiangli Fan

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3203-3212 DOI: 10.6023/cjoc20205022

Abstract( 72) HTML( 10) PDF(2693KB)( 63 )

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Recent Advances in Selective C—H Bond Functionalization of Amines Through Hydrogen Atom Transfer (HAT) Process

Huanle Li, Qi Pan, Shaojie Lou, Yangjie Mao, Danqian Xu

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3213-3243 DOI: 10.6023/cjoc202503010

Abstract( 281) HTML( 24) PDF(1580KB)( 2461 )

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Research Progress of Low-Coordinate Phosphenium Ions Compounds

Tianqing Zhang, Xiuming Wu, Congcong Wang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3244-3254 DOI: 10.6023/cjoc202502021

Abstract( 131) HTML( 10) PDF(5108KB)( 79 )

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Advances in Synthesis Methods of Quinoline and Isoquinoline Derivatives

Liping Guan, Zhiqi Lin, Chaohua Fang, Qiushi Wang, Zhiyang Fu, Bin Zhang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3255-3288 DOI: 10.6023/cjoc202502036

Abstract( 199) HTML( 5) PDF(1409KB)( 812 )

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Applications of Palladium-Catalyzed Cascade Reactions in Total Synthesis of Complex Natural Products with Quaternary Carbon Centers

Qianqian Zhao, Peiyao Wei, Sundian Liu, Boxin Zhang, Chengyuan Liang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3289-3300 DOI: 10.6023/cjoc202502022

Abstract( 132) HTML( 6) PDF(853KB)( 165 )

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Advances in Chemoselective Recognition of Amino Acids by Schiff Base Fluorescent Probes

Aopei Peng, Yang Li, Yuanyuan Zhu, Guangwen Wu, Shuangxi Gu

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3301-3313 DOI: 10.6023/cjoc202503015

Abstract( 170) HTML( 9) PDF(8525KB)( 114 )

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Recent Progress in the Application of Biomimetic Material Polydopamine in Organic Conversion

Wei Yang, Bingbing Wang, Xiaohui Xu, Zhong Sun, Cuiman Tang, Jiaqi Liu

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3314-3325 DOI: 10.6023/cjoc202502024

Abstract( 321) HTML( 2) PDF(911KB)( 214 )

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ARTICLES

Ir/f-Amphox-Catalyzed Asymmetric Hydrogenation of 1-(Pyridin-2-yl)ketones to Chiral Pyridyl Alcohols^★

Qishu Chen, Bo Yang, Qiwei Lang, Xiaobing Ding, Xiuxiu Li, Xumu Zhang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3326-3334 DOI: 10.6023/cjoc202505032

Abstract( 112) HTML( 4) PDF(619KB)( 111 )

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A Novel Synthetic Process of Daprodustat^★

Zhiyong Xu, Xiaohui Lin, Yuanyuan Zhu, Shuangshuang Zhang, Jiao Long, Shuangxi Gu

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3335-3342 DOI: 10.6023/cjoc202504010

Abstract( 162) HTML( 6) PDF(578KB)( 118 )

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Visible-Light-Induced Diborylation to Access gem-Diborylalkanes^★

Bowen Ren, Tongchang Fang, Chao Liu

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3343-3350 DOI: 10.6023/cjoc202504018

Abstract( 210) HTML( 6) PDF(781KB)( 128 )

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A Sterically Hindered Phosphorus Ligand for Palladium-Catalyzed Sterically Hindered Aryl-Alkyl Coupling Reaction^★

Nan Wang, Wenjun Tang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3351-3360 DOI: 10.6023/cjoc202506005

Abstract( 203) HTML( 16) PDF(1012KB)( 166 )

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Alumina-Promoted Michael Addition of Imidazo[1,2-a]pyridines with α,β-Unsaturated Ketones

Yadong Sun, Hai Zhou, Tucai Zheng, Shoucai Wang, Fanghua Ji

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3361-3369 DOI: 10.6023/cjoc202503008

Abstract( 105) HTML( 2) PDF(550KB)( 73 )

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A New Semi-synthesis Route of Belotecan

Yukai Zhang, Yufeng Liang, Qingrong Qi

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3370-3377 DOI: 10.6023/cjoc202501018

Abstract( 224) HTML( 1) PDF(590KB)( 222 )

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Construction and Antifungal Activity Study of Trifluoroacetyl Substituted Spiro Indolinone-Hexahydropyrrolizine Derivatives

Rui Zhang, Yin Zhang, Wenjuan Li, Xiaoqiang Han, Jixing Zhao

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3378-3391 DOI: 10.6023/cjoc202503011

Abstract( 127) HTML( 1) PDF(676KB)( 54 )

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Design, Synthesis, and Electroluminescent Performance Study of meta-Terphenyl-Modified Thermally Activated Delayed Fluorescence Host

Junyu Zhu, Jinlong Liao, Lei Dai, Wencheng Chen, Yanping Huo

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3390-3400 DOI: 10.6023/cjoc202503019

Abstract( 119) HTML( 7) PDF(5702KB)( 380 )

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Cr-Catalyzed Reductive Cross-Coupling of Trifluoromethyl Alkenes

Wen Xu, Meiming Luo, Xiaoming Zeng

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3401-3411 DOI: 10.6023/cjoc202505016

Abstract( 225) HTML( 6) PDF(550KB)( 137 )

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Copper Catalyzed C—O Coupling for the Preparation of m-Phenoxybenzaldehyde

Chenxu Jia, Conghao An, Jun Huang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3412-3419 DOI: 10.6023/cjoc202502035

Abstract( 142) HTML( 2) PDF(1661KB)( 75 )

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Organic Base-Promoted [2+3] Annulation of Arylglyoxal Monohydrates with Allyl Phosphonium Salts: Efficient Syntheses of Cyclopentenones

Sen Zhang, Lingyun Jiang, Yu Xin, Nianyu Huang, Nengzhong Wang

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3420-3428 DOI: 10.6023/cjoc202502010

Abstract( 425) HTML( 3) PDF(659KB)( 141 )

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4-Dimethylamino-pyridine (DMAP)-Promoted [5＋1] Annulation of Isoquinolinium Zwitterions with α-Bromophenones: An Efficient Approach to Hydrogenated 1,4-Thiazino[2,3-a]isoquinoline Tricyclic Derivatives

Yanan Cai, Xiangtai Meng

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3429-3440 DOI: 10.6023/cjoc202502008

Abstract( 128) HTML( 4) PDF(810KB)( 104 )

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Design and Synthesis of Donor-Acceptor-Donor (D-A-D) Type Aromatic Ketones for Photocatalytic C(sp³)—H Coupling Reactions

Hui Zhu, Peng Wu, Chenming Zhong, Shuming Li, Gang Lin, Xuefen Liu, Shuping Luo

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3441-3449 DOI: 10.6023/cjoc202501013

Abstract( 131) HTML( 1) PDF(584KB)( 50 )

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A Multifunctional Porous Organic Polymer Supported Pd Nanoparticle Catalyst for Hydrocarboxylation of Alkynes

Zhiqi Yu, Canyuan Chen, Jiayi Han, Jianhu Zhou, Linxuan Wang, Meie Yue, Xiaofei Jia

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3450-3457 DOI: 10.6023/cjoc202503012

Abstract( 86) HTML( 5) PDF(13644KB)( 37 )

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Silver/Ganphos-Catalyzed Enantioselective [3＋2] Cycloadditions of Azomethine Ylides: Access to the Spirocyclic Scaffolds

Mengya Xu, Yifan Li, Yue Wang, Ruiping Han, Er-Qing Li

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3458-3468 DOI: 10.6023/cjoc202502019

Abstract( 282) HTML( 2) PDF(852KB)( 111 )

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Iodine-Catalyzed Intermolecular Cyclopropanation of Olefins with Active Methylene Compounds

Yuhan Zhao, Huimin Ma, Shulin Ge, Lingbin Kong

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3469-3477 DOI: 10.6023/cjoc202502038

Abstract( 183) HTML( 6) PDF(564KB)( 106 )

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Formal Synthesis of Dydrogesterone: A Milder Dearomatization Strategy^★

Hongmiao Yao, Shaodong Wang, Xinxin Yuan, Qianding Zeng, Hai Jiang, Yiyong Zou, Jiangmeng Ren, Yusong Zhang, Bu-Bing Zeng

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3478-3485 DOI: 10.6023/cjoc202502033

Abstract( 215) HTML( 5) PDF(565KB)( 131 )

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A Rare Sesquiterpene from Hawk Tea

Dongyang Guo, Jingxian Cong, Maosheng Zhang, Minjian Dong, Guangxiang Liang, Chengxin Sun, Wenxi Wu, Shiji Xiao

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3486-3489 DOI: 10.6023/cjoc202502012

Abstract( 120) HTML( 2) PDF(737KB)( 89 )

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HIGHLIGHTS

Nickel-Catalyzed Enantioselective Reductive Cross-Coupling of Amino Alcohol-Derived Sulfonates

Fen Hu, Wangqing Kong

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3490-3491 DOI: 10.6023/cjoc202500020

Abstract( 71) HTML( 7) PDF(469KB)( 38 )

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Photoinduced 1,2-Carbonyl Migration and 1,3-Difunctionalization of β,γ-Unsaturated Ketones

Shuji Gao, Xueqiang Chu

Chinese Journal of Organic Chemistry 2025, 45 (9), pp 3492-3494 DOI: 10.6023/cjoc202500021

Abstract( 56) HTML( 2) PDF(421KB)( 47 )

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