Publications

2024

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, jacs.4c03634. 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, 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

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

C—F Bond Insertion into Indoles with CHBr₂F: An Efficient Method to Synthesize Fluorinated Quinolines and Quinolones

Chao Li, Lei Chen, Hongye Wang, Zixi Yan, Bin Lyu, Weiping Lyu, Changwei Jiang, Dehua Lu, Jiaxing Li, Ning Jiao, Song Song*

Chin. J. Chem. 2024, 42 (10), 1128–1132. DOI: 10.1002/cjoc.202400033

C—F Bond Insertion into Indoles with CHBr<sub>2</sub>F: An Efficient Method to Synthesize Fluorinated Quinolines and Quinolones

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

Organocatalytic Deoxyhalogenation of Alcohols with Inorganic Halides

Weijin Wang, Hongye Wang, Rongheng Dai, Yachong Wang, Zhaoting Li, Xiaoxue Yang, Bin Lu, Ning Jiao, Song Song*

ACS Catal. 2023, 13 (13), 9033–9040. DOI: 10.1021/acscatal.3c02078

Organocatalytic Deoxyhalogenation of Alcohols with Inorganic Halides

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

An Efficient and Mild Oxidative Approach from Thiols to Sulfonyl Derivatives with DMSO/HBr

Hongye Wang, Zhaoting Li, Rongheng Dai, Ning Jiao, Song Song*

Chem. Sci. 2023, 14 (45), 13228–13234. DOI: 10.1039/d3sc04945k

An Efficient and Mild Oxidative Approach from Thiols to Sulfonyl Derivatives with DMSO/HBr

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

Electrophilic Amidomethylation of Arenes with DMSO/MeCN Reagents

Hongliang Zhang, Weijin Wang, Bingding Wang, Hui Tan, Ning Jiao*, Song Song*

Org. Chem. Front. 2022, 9 (9), 2430–2437. DOI: 10.1039/d2qo00181k

Electrophilic Amidomethylation of Arenes with DMSO/MeCN Reagents

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

Cleaving Arene Rings for Acyclic Alkenylnitrile Synthesis

Oxoammonium Salts Are Catalysing Efficient and Selective Halogenation of Olefins, Alkynes and Aromatics

Weijin Wang, Xinyao Li, Xiaoxue Yang, Lingsheng Ai, Zhiwen Gong, Ning Jiao, Song Song*

Nat. Commun. 2021, 12 (1), 3873. DOI: 10.1038/s41467-021-24174-w

Oxoammonium Salts Are Catalysing Efficient and Selective Halogenation of Olefins, Alkynes and Aromatics

Cu(I)-Catalyzed [2+2+1] Cycloaddition of Amines, Alkynes, and Ketenes: An Umpolung and Regioselective Approach to Full-Substituted β-Pyrrolinones

Hao Wu, Xinyao Li, Zixi Yan, Nana Ma, Song Song*, Guisheng Zhang*, Ning Jiao*

Org. Lett. 2021, 23 (3), 762–766. DOI: 10.1021/acs.orglett.0c03991

Cu(I)-Catalyzed [2+2+1] Cycloaddition of Amines, Alkynes, and Ketenes: An Umpolung and Regioselective Approach to Full-Substituted β-Pyrrolinones

N‐Heterocyclic Carbene Catalyzed Ester Synthesis from Organic Halides through Incorporation of Oxygen Atoms from Air

Hui Tan, Shenan Wang, Zixi Yan, Jianzhong Liu, Jialiang Wei, Song Song*, Ning Jiao*

Angew. Chem. Int. Ed. 2021, 60 (4), 2140–2144. DOI: 10.1002/anie.202011039

N‐Heterocyclic Carbene Catalyzed Ester Synthesis from Organic Halides through Incorporation of Oxygen Atoms from Air

Electrochemical Oxidation Induced Selective C–C Bond Cleavage

Shihui Shi, Yujie Liang, Ning Jiao*

Chem. Rev. 2021, 121 (1), 485–505. DOI: 10.1021/acs.chemrev.0c00335

Electrochemical Oxidation Induced Selective C–C Bond Cleavage

Electrochemically Induced Nickel Catalysis for Oxygenation Reactions with Water

Yujie Liang, Shihui Shi, Rui Jin, Xu Qiu, Jialiang Wei, Hui Tan, Xue Jiang, Xiaomeng Shi, Song Song, Ning Jiao*

Nat. Catal. 2021, 4 (2), 116–123. DOI: 10.1038/s41929-020-00559-w

Electrochemically Induced Nickel Catalysis for Oxygenation Reactions with Water

Molecular Oxygen-Mediated Oxygenation Reactions Involving Radicals

Conghui Tang, Xu Qiu, Zengrui Cheng, Ning Jiao*

Chem. Soc. Rev. 2021, 50 (14), 8067–8101. DOI: 10.1039/d1cs00242b

Molecular Oxygen-Mediated Oxygenation Reactions Involving Radicals

2020

Nitromethane-Enabled Fluorination of Styrenes and Arenes

Weijin Wang, Tongyu Huo, Xinyi Zhao, Qixue Qin, Yujie Liang, Song Song*, Guosheng Liu*, Ning Jiao*.

CCS Chemistry 2020, 2 (6), 566–575. DOI: 10.31635/ccschem.020.202000172

Nitromethane-Enabled Fluorination of Styrenes and Arenes

DMSO‐Enabled Selective Radical O−H Activation of 1,3(4)‐Diols

Yuchao Zhu, Ziyao Zhang, Rui Jin, Jianzhong Liu, Guoquan Liu, Bing Han, Ning Jiao*

Angew. Chem. Int. Ed. 2020, 59 (45), 19851–19856. DOI: 10.1002/anie.202007187

DMSO‐Enabled Selective Radical O−H Activation of 1,3(4)‐Diols

Efficient Pd‐Catalyzed C–H Oxidative Bromination of Arenes with Dimethyl Sulfoxide and Hydrobromic Acid

Yizhi Yuan, Yujie Liang, Shihui Shi, Yufeng Liang, Ning Jiao*

Chin. J. Chem. 2020, 38 (11), 1245–1251. DOI: 10.1002/cjoc.202000055

Efficient Pd‐Catalyzed C–H Oxidative Bromination of Arenes with Dimethyl Sulfoxide and Hydrobromic Acid

Rational Modification, Synthesis and Biological Evaluation of 3,4-Dihydroquinoxalin-2(1H)-One Derivatives as Potent and Selective c-Jun N-Terminal Kinase 3 (JNK3) Inhibitors

Xiaodong Dou, Huixia Huang, Lan Jiang, Guiwang Zhu, Hongwei Jin, Ning Jiao, Liangren Zhang*, Zhenming Liu*, Lihe Zhang

Eur. J. Med. Chem. 2020, 201, 112445. DOI: 10.1016/j.ejmech.2020.112445

Rational Modification, Synthesis and Biological Evaluation of 3,4-Dihydroquinoxalin-2(1H)-One Derivatives as Potent and Selective c-Jun N-Terminal Kinase 3 (JNK3) Inhibitors

Nitromethane as a Nitrogen Donor in Schmidt-Type Formation of Amides and Nitriles

Jianzhong Liu, Cheng Zhang, Ziyao Zhang, Xiaojin Wen, Xiaodong Dou, Jialiang Wei, Xu Qiu, Song Song*, Ning Jiao*

Science 2020, 367 (6475), 281–285. DOI: 10.1126/science.aay9501

Nitromethane as a Nitrogen Donor in Schmidt-Type Formation of Amides and Nitriles

From Hydroxylamines to Anilines via Trifluoroacetic Anhydride (TFAA) Assisted Stieglitz Rearrangement

Xiao Luo, Ning Jiao*

Acta Chim. Sinica 2020, 78 (8), 758. DOI: 10.6023/A20050191

From Hydroxylamines to Anilines via Trifluoroacetic Anhydride (TFAA) Assisted Stieglitz Rearrangement

Selective Dealkenylative Functionalization of Styrenes via C-C Bond Cleavage

Jianzhong Liu, Jun Pan, Xiao Luo, Xu Qiu, Cheng Zhang, Ning Jiao*

Research 2020, 2020, 2020/7947029. DOI: 10.34133/2020/7947029

Selective Dealkenylative Functionalization of Styrenes via C-C Bond Cleavage

Deconstructive Reorganization: De Novo Synthesis of Hydroxylated Benzofurans

Ziyao Zhang, Ning Jiao*

Chinese J. Org. Chem. 2020, 40 (6), 1790. DOI: 10.6023/cjoc202000031

Deconstructive Reorganization: De Novo Synthesis of Hydroxylated Benzofurans

Intramolecular Csp³–H/C–C Bond Amination of Alkyl Azides for the Selective Synthesis of Cyclic Imines and Tertiary Amines

Xiaojin Wen, Xinyao Li, Xiao Luo, Weijin Wang, Song Song*, Ning Jiao*

Chem. Sci. 2020, 11 (17), 4482–4487. DOI: 10.1039/c9sc05522c

Intramolecular Csp<sup>3</sup>–H/C–C Bond Amination of Alkyl Azides for the Selective Synthesis of Cyclic Imines and Tertiary Amines

2019

DMSO-Catalysed Late-Stage Chlorination of (Hetero)Arenes

Song Song, Xinyao Li, Jialiang Wei, Weijin Wang, Yiqun Zhang, Lingsheng Ai, Yuchao Zhu, Xiaomeng Shi, Xiaohui Zhang, Ning Jiao*

Nat. Catal. 2019, 3 (2), 107–115. DOI: 10.1038/s41929-019-0398-0