Publications

2025

From Alkylarenes to α-Amino Acid Derivatives via C-Difunctionalization

Xi Wang, Jianzhong Liu, Zengrui Cheng, Teng Wang, Jing Peng, Junhong Meng, Yilei Huang, Qi Sun*, Ning Jiao*

J. Am. Chem. Soc. 2025, jacs.5c14247. DOI: 10.1021/jacs.5c14247

From Alkylarenes to α-Amino Acid Derivatives via C-Difunctionalization

Aerobic oxidative synthesis of o-phenylenediamines from cyclohexanones

Yichen Sun^†, Shuyuan Tang^†, Binzhi Zhao^† and Ning Jiao*

Green Chem. 2025, 27 (27), 8120–8125. DOI: 10.1039/D5GC01786F

Aerobic oxidative synthesis of o-phenylenediamines from cyclohexanones

Bidentate N-ligand-assisted gold redox catalysis with hydrogen peroxide

Hongwei Shi, Matthias Rudolph, Jun Li, Yu Tian, Martin C. Dietl, Hadil Alshurafa, Yaowen Liu, Tao Wang, Henrik Habeck, Philipp M. Stein, Petra Krämer, Frank Rominger, Thomas Oeser, Ning Jiao* & A. Stephen K. Hashmi*

Nat. Chem. 2025, 17 (6), 822–834. DOI: 10.1038/s41557-025-01835-7

Bidentate N-ligand-assisted gold redox catalysis with hydrogen peroxide

Catalytic remodeling of complex alkenes to oxonitriles through C=C double bond deconstruction

Zengrui Cheng^†, Kaimeng Huang^†, Chen Wang^†, Lili Chen^†, Xinyao Li, Zhibin Hu, Xinyuan Shan, Pengfei Cao, Haofeng Sun, Wei Chen, Chenhao Li, Ziyao Zhang, Hui Tan, Xue Jiang, Guikai Zhang, Zhongying Zhang, Min Lin, Liang Wang, Anmin Zheng, Changjiu Xia*, Teng Wang, Song Song, Xingtian Shu, Ning Jiao*

Science 2025, 387 (6738), 1083-1090. DOI: 10.1126/science.adq8918

Catalytic remodeling of complex alkenes to oxonitriles through C=C double bond deconstruction

Molecular Ring Remodeling through C–C Bond Cleavage

Zengrui Cheng^†, Zhibin Hu^†, Ning Jiao*

Acc. Chem. Res. 2025, 58 (6), 1003–1022. DOI: 10.1021/acs.accounts.4c00846

Molecular Ring Remodeling through C–C Bond Cleavage

2024

Direct oxygen insertion into C-C bond of styrenes with air

Qixue Qin*, Liang Zhang, Jialiang Wei, Xu Qiu, Shuanghong Hao, Xiao-De An, Ning Jiao*

Nat. Commun. 2024, 15, 9015. DOI: 10.1038/s41467-024-53266-6

Direct oxygen insertion into C-C bond of styrenes with air

Late-Stage Halogenation of Complex Substrates with Readily Available Halogenating Reagents

Weijin Wang, Song Song*, Ning Jiao*

Acc. Chem. Res. 2024, 57 (21), 3161–3181. DOI: 10.1021/acs.accounts.4c00501

Late-Stage Halogenation of Complex Substrates with Readily Available Halogenating Reagents

Selective Upcycling of Polyolefins into High-Value Nitrogenated Chemicals

Binzhi Zhao, Zhibin Hu, Yichen Sun, Rehemuhali Hajiayi, Teng Wang, Ning Jiao*

J. Am. Chem. Soc. 2024, 146 (42), 28605–28611. DOI: 10.1021/jacs.4c07965

Selective Upcycling of Polyolefins into High-Value Nitrogenated Chemicals

Selective nitrogen insertion into aryl alkanes

Zheng Zhang, Qi Li, Zengrui Cheng, Ning Jiao*, Chun Zhang*

Nat. Commun. 2024, 15, 6016. DOI: 10.1038/s41467-024-50383-0

Selective nitrogen insertion into aryl alkanes

Research progress on GPX4 targeted compounds

Bingru Li^†, Keguang Cheng^†, Tzumei Wang, Xing Peng, Ping Xu, Guoquan Liu, Dong Xue, Ning Jiao, Chao Wang*

Eur. J. Med. Chem. 2024, 274, 116548. DOI: 10.1016/j.ejmech.2024.116548

Research progress on GPX4 targeted compounds

Carbene-Assisted Arene Ring-Opening

Zengrui Cheng^†, Haoran Xu^†, Zhibin Hu, Minghui Zhu, K. N. Houk*, Xiao-Song Xue*, Ning Jiao*

J. Am. Chem. Soc. 2024, 146 (25), 16963–16970. DOI: 10.1021/jacs.4c03634

Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation

Xiaodong Dou^†, Tongyu Huo^†, Yameng Liu^†, Zichen Pang, Lingyu Su, Xinyi Zhao, Xing Peng, Zhenming Liu, Liangren Zhang, Ning Jiao*

Eur. J. Med. Chem. 2024, 269, 116323. DOI: 10.1016/j.ejmech.2024.116323

Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation

Selective Ring-Opening Amination of Isochromans and Tetrahydroisoquinolines

Changhao Niu, Zheng Zhang, Qi Li, Zengrui Cheng, Ning Jiao*, Chun Zhang*

Angew. Chem. Int. Ed. 2024, 63 (17), e202401318. DOI: 10.1002/anie.202401318

Selective Ring-Opening Amination of Isochromans and Tetrahydroisoquinolines

Dioxygen compatible electron donor-acceptor catalytic system and its enabled aerobic oxygenation

Jialiang Wei, Junhong Meng, Caifang Zhang, Yameng Liu, Ning Jiao*

Nat. Commun. 2024, 15, 1886. DOI: 10.1038/s41467-024-45866-z

Dioxygen compatible electron donor-acceptor catalytic system and its enabled aerobic oxygenation

Catalytic Conversion of Mixed Polyolefins under Mild Atmospheric Pressure

Binzhi Zhao, Hui Tan, Jie Yang, Xiaohui Zhang, Zidi Yu, Hanli Sun, Jialiang Wei, Xinyi Zhao, Yufeng Zhang, Lili Chen, Dali Yang, Jin Deng, Yao Fu, Zheng Huang, Ning Jiao*

The Innovation 2024, 5 (2), 100586. DOI: 10.1016/j.xinn.2024.100586

Catalytic Conversion of Mixed Polyolefins under Mild Atmospheric Pressure

Organic Synthesis through Radical Innovation: Frustrated Radical Pairs

Zhibin Hu, Zengrui Cheng, Ning Jiao*

Chin. J. Chem. 2024, 42 (10), 1157–1160. DOI: 10.1002/cjoc.202300665

Organic Synthesis through Radical Innovation: Frustrated Radical Pairs

A Catalytic Method to Activate Nitromethane by the Cooperation of Homo- and Heterogeneous Catalysis

Weijin Wang, Jianzhong Liu, Licheng Yang, Song Song, Ning Jiao*

Angew. Chem. Int. Ed. 2024, 63 (7), e202312354. DOI: 10.1002/anie.202312354

A Catalytic Method to Activate Nitromethane by the Cooperation of Homo- and Heterogeneous Catalysis

Nitromethane Assisted Brønsted Acid Catalyzed Regioselective Halogenation of Alkyl Aromatics

Shihui Shi, Song Song, Ning Jiao*

Mol. Catal. 2024, 553, 113777. DOI: 10.1016/j.mcat.2023.113777

Nitromethane Assisted Brønsted Acid Catalyzed Regioselective Halogenation of Alkyl Aromatics

Discovery of 3-Oxo-1,2,3,4-Tetrahydropyrido[1,2-a]Pyrazin Derivatives as SARS-CoV-2 Main Protease Inhibitors through Virtual Screening and Biological Evaluation

Xiaodong Dou^†, Qi Sun^†, Yameng Liu^†, Yangbin Lu, Caifang Zhang, Guofeng Xu, Yue Xu, Tongyu Huo, Xinyi Zhao, Lingyu Su, Yihong Xing, Luhua Lai*, Ning Jiao*

Bioorg. Med. Chem. Lett. 2024, 97, 129547. DOI: 10.1016/j.bmcl.2023.129547

Discovery of 3-Oxo-1,2,3,4-Tetrahydropyrido[1,2-a]Pyrazin Derivatives as SARS-CoV-2 Main Protease Inhibitors through Virtual Screening and Biological Evaluation

2023

Carbon–Carbon Bond Cleavage for Late-Stage Functionalization

Yufeng Liang*, Muhammad Bilal, Leyu Tang, Tianzhang Wang, Yuqiu Guan, Zengrui Cheng, Minghui Zhu, Jialiang Wei, Ning Jiao*

Chem. Rev. 2023, 123 (22), 12313–12370. DOI: 10.1021/acs.chemrev.3c00219

Carbon–Carbon Bond Cleavage for Late-Stage Functionalization

Regioselective Synthesis of 4-Functionalized Pyridines

Chao Li^†, Zixi Yan^†, Bingding Wang, Jiaxing Li, Weiping Lyu, Zhixing Wang, Ning Jiao*, Song Song*

Chem 2023, S2451929423005223. DOI: 10.1016/j.chempr.2023.10.015

Regioselective Synthesis of 4-Functionalized Pyridines

Late-Stage Modification of Bioactive Compounds: Improving Druggability through Efficient Molecular Editing

Tongyu Huo^†, Xinyi Zhao^†, Zengrui Cheng, Jialiang Wei, Minghui Zhu, Xiaodong Dou*, Ning Jiao*

Acta Pharm. Sin. B 2023, S2211383523004446. DOI: 10.1016/j.apsb.2023.11.021

Late-Stage Modification of Bioactive Compounds: Improving Druggability through Efficient Molecular Editing

Functional Screening and Rational Design of Compounds Targeting GPR132 to Treat Diabetes

Jiale Wang^†, Xiaodong Dou^†, Jie Cheng^†, Mingxin Gao^†, Guofeng Xu^†, Wei Ding^†, Jinhui Ding^†, Yu Li, Sihan Wang, Zhaowei Ji, Xinyi Zhao, Tongyu Huo, Caifang Zhang, Yameng Liu, Xueying Sha, Jiarui Gao, Wenhui Zhang, Yong Hao, Cheng Zhang, Jinpeng Sun*, Ning Jiao*, Xiao Yu*

Nat. Metab. 2023, 5 (10), 1726–1746. DOI: 10.1038/s42255-023-00899-4

Functional Screening and Rational Design of Compounds Targeting GPR132 to Treat Diabetes

Aminotetrazole Synthesis from Secondary Amides by C–C Bond Nitrogenation

Cheng Zhang, Jianzhong Liu, Zengrui Cheng, Junhua Li, Song Song, Ning Jiao*

Synlett 2023, 34 (12), 1534–1538. DOI: 10.1055/a-2006-4548

Aminotetrazole Synthesis from Secondary Amides by C–C Bond Nitrogenation

Nitrogenation of Amides via C–C and C–N Bond Cleavage

Minghui Zhu, Zengrui Cheng, Jialiang Wei, Hui Tan, Ning Jiao*

CCS Chemistry 2023, 5 (5), 1061–1068. DOI: 10.31635/ccschem.022.202202585

Nitrogenation of Amides via C–C and C–N Bond Cleavage

Recent Applications of Trifluoromethanesulfonic Anhydride in Organic Synthesis

Qixue Qin^†, Zengrui Cheng^†, Ning Jiao*

Angew. Chem. Int. Ed. 2023, 62 (10), e202215008. DOI: 10.1002/anie.202215008

Recent Applications of Trifluoromethanesulfonic Anhydride in Organic Synthesis

Rhodium-Catalyzed Transannulation of 1,2,3‐THIAZOLES with Alkynes for the Direct Synthesis of Thiochromenones

Jun Pan^†, Ziyao Zhang^†, Lili Chen, Ning Jiao*

Chin. J. Chem. 2023, 41 (5), 509–513. DOI: 10.1002/cjoc.202200603

Rhodium-Catalyzed Transannulation of 1,2,3‐THIAZOLES with Alkynes for the Direct Synthesis of Thiochromenones

Alternative Method to Baeyer–Villiger Oxidation of Cyclobutenones Using I₂/DMSO Catalytic Systems

Yichen Sun, Zhibin Hu, Jing Peng, Qixue Qin*, Ning Jiao*

Green Chem. 2023, 25 (18), 7079–7083. DOI: 10.1039/d3gc01756g

Alternative Method to Baeyer–Villiger Oxidation of Cyclobutenones Using I<sub>2</sub>/DMSO Catalytic Systems

2022

Discovery of 2-(Furan-2-Ylmethylene)Hydrazine-1-Carbothioamide Derivatives as Novel Inhibitors of SARS-CoV-2 Main Protease

Xiaodong Dou^†, Qi Sun^†, Guofeng Xu^†, Yameng Liu, Caifang Zhang, Bingding Wang, Yangbin Lu, Zheng Guo, Lingyu Su, Tongyu Huo, Xinyi Zhao, Chen Wang, Zhongtian Yu, Song Song, Liangren Zhang, Zhenming Liu, Luhua Lai*, Ning Jiao*

Eur. J. Med. Chem. 2022, 238, 114508. DOI: 10.1016/j.ejmech.2022.114508

Discovery of 2-(Furan-2-Ylmethylene)Hydrazine-1-Carbothioamide Derivatives as Novel Inhibitors of SARS-CoV-2 Main Protease

Catalytic Electrophilic Halogenation of Arenes with Electron-Withdrawing Substituents

Weijin Wang^†, Xiaoxue Yang^†, Rongheng Dai, Zixi Yan, Jialiang Wei, Xiaodong Dou, Xu Qiu, Hongliang Zhang, Chen Wang, Yameng Liu, Song Song*, Ning Jiao*

J. Am. Chem. Soc. 2022, 144 (29), 13415–13425. DOI: 10.1021/jacs.2c06440

Catalytic Electrophilic Halogenation of Arenes with Electron-Withdrawing Substituents

Discovery of Novel Ataxia Telangiectasia Mutated (ATM) Kinase Modulators: Computational Simulation, Biological Evaluation and Cancer Combinational Chemotherapy Study

Xiaodong Dou^†, Xiaojiao Sun^†, Huixia Huang^†, Lan Jiang^†, Zefang Jin, Yameng Liu, Yang Zou, Zhongtang Li, Guiwang Zhu, Hongwei Jin, Ning Jiao, Liangren Zhang*, Zhenming Liu*, Lihe Zhang

Eur. J. Med. Chem. 2022, 233, 114196. DOI: 10.1016/j.ejmech.2022.114196

Discovery of Novel Ataxia Telangiectasia Mutated (ATM) Kinase Modulators: Computational Simulation, Biological Evaluation and Cancer Combinational Chemotherapy Study

Selective Desaturation of Amides: A Direct Approach to Enamides

Xinwei Li^†, Zengrui Cheng^†, Jianzhong Liu, Ziyao Zhang, Song Song*, Ning Jiao*

Chem. Sci. 2022, 13 (31), 9056–9061. DOI: 10.1039/d2sc02210a

Selective Desaturation of Amides: A Direct Approach to Enamides

2021

Selective Carbon‐Carbon Bond Amination with Redox‐Active Aminating Reagents: A Direct Approach to Anilines

Xu Qiu^†, Yachong Wang^†, Lingyu Su, Rui Jin, Song Song, Qixue Qin, Junhua Li, Baoning Zong, Ning Jiao*

Chin. J. Chem. 2021, 39 (11), 3011–3016. DOI: 10.1002/cjoc.202100430

Selective Carbon‐Carbon Bond Amination with Redox‐Active Aminating Reagents: A Direct Approach to Anilines

Cleaving Arene Rings for Acyclic Alkenylnitrile Synthesis

Xu Qiu^†, Yueqian Sang^†, Hao Wu^†, Xiao-Song Xue, Zixi Yan, Yachong Wang, Zengrui Cheng, Xiaoyang Wang, Hui Tan, Song Song, Guisheng Zhang, Xiaohui Zhang, K. N. Houk*, Ning Jiao*

Nature 2021, 597 (7874), 64–69. DOI: 10.1038/s41586-021-03801-y