中国药科大学

林爱俊(Aijun Lin)，博士，1982年出生，江苏金坛人。中国药科大学药学院副教授（药物化学），硕士生导师。2005-2011年南京大学化学化工学院有机化学专业硕/博连读，获博士学位。2011-2012年，南京大学化学化工学院/生命科学学院博士后。2012-2014年，美国德州农工大学（TexasA&MUniversity）化学系博士后。2014年4月作为海外高层次引进人才进入中国药科大学药学院工作。博士论文《有机催化不对称碳杂键形成反应研究》获2012年Eli Lilly Asia Outstanding Thesis Award。至今已在Angewandte Chemie International Edition, Chemical Communication, Organic Letters, Chemistry - A European Journal, Advanced Synthesis & Catalysis, The Journal of Organic Chemistry等国际著名期刊上发表SCI论文40多篇。参与编写专著一章节：林爱俊、朱成建，第9章“串联的不对称催化反应”，《不对称催化新概念与新方法》，丁奎岭、范青华主编，化学工业出版社，2009年出版。目前主持国家自然科学基金青年项目1项，江苏省自然科学基金青年项目1项、中国药科大学高层次引进人才启动经费项目。热忱欢迎本科生、硕士研究生加入本课题组从事基础科学研究。

联系方式

Lab:玄武门校区科研大楼1808和1812室

Address：南京市童家巷24号科研大楼1812室，中国药科大学，邮编210009

Email：ajlin@cpu.edu.cnorlinaijun1982@sina.com

主要研究

1.有机合成方法学研究(不对称催化与合成、惰性C-H键官能化、协同催化、多组分串联反应)，重点研究不同合成方法在复杂药物分子和活性先导化合物中的应用

2.目标导向的功能性杂环化合物的设计与合成，生物活性和毒性测试与评价，探索并发现潜在药物分子骨架

3.生物活性天然化合物及其类似物合成、结构修饰以及基于天然活性骨架的创新药物研发

Selected publications:

1、Kuo Gai, Xinxin Fang, Xuanyi Li, Jinyi Xu, Xiaoming Wu, Aijun Lin* and Hequan Yao*, “Synthesis of Spiro[2.5]octa-4,7-dien-6-one with Consecutive Quarternary Centers via 1,6-Conjugate Addition Induced Dearomatization of para-Quinone Methides.” Chem Commun, 2015, accepted.

2、Xuanyi Li, Kuo Gai, Zhenbo Yuan, Jie Wu, Aijun Lin* and Hequan Yao* “Organocatalyzed formal [4+2] cycloaddition of in situ generated azoalkenes with aryl acetic acids: an efficient approach to the synthesis of 4,5-dihydropyridazin-3(2H)-ones.” Adv. Synth. Catal. 2015, in revision.

3、Zhenbo Yuan, Xinxin Fang, Xuanyi Li, Jie Wu, Aijun Lin* and Hequan Yao* “1,6-Conjugated Addition Mediated Dearomatization: Approach to Spiro[2.5]octa-4,7-dien-6-one.” Journal of Organic Chemistry, 2015, in revision.

4、Youla Su, Shang Gao, Yue Huang, Aijun Lin* and Hequan Yao* “Solvent-controlled C2/C5-regiodivergent alkenylation of pyrroles.” Chem. Eur. J., 2015, accepted.

5、Peng Sun, Youzhi Wu, Tie Yang, Xiaoming Wu, Jinyi Xu, Aijun Lin,* Hequan Yao*. “Synthesis of Heterocycle-fused-Pyridine N-Oxides from Oximes and Diazo Compounds via Rh(III)-Catalyzed C-H Activation and Annulation. ” Adv. Synth. Catal. 2015, in press.

6、Xuebing Chen, Peng Sun, Jinyi Xu, Xiaoming Wu, Lingyi Kong, Hequan Yao* and Aijun Lin*. “Construction of indoloquinolinones via Pd(II)-catalyzed tandem C-C/C-N bond formation: application to the total synthesis of isocryptolepine.” Tetrahedron Lett，2014, 55, 7114-7117.

7、Youla Su, Haipin Zhou, Jiaxuan Chen, Jinyi Xu, Xiaoming Wu, Aijun Lin* and Hequan Yao*. “Solvent-controlled Switchable C-H Alkenylation of 4-Aryl 1H-pyrrole 3-carboxylates: Application to the Total Synthesis of (±)-Rhazinilam.” Org. Lett. 2014, 16, 4884-4887.

8、Aijun Lin, Zhi-wei Zhang and Jiong Yang.* “Iron-Catalyzed Reductive Cyclization of 1,6-Enynes.” Org. Lett. 2014, 16, 386-389.

9、Aijun Lin, C. Bryan Huehls, Jiong Yang. “Recent advances in C-H fluorination.” Org. Chem. Front. 2014, 1, 434-438.

10、Haibin Mao,a Aijun Lin,a Zhongkai Tang, Hongwen Hu, Chengjian Zhu*, Yixiang Cheng.* “Organocatalytic One-pot Synthesis of Highly Substituted Pyridazines from Morita-Baylis-Hillman Carbonates and Diazo Compounds.” Chem. Eur. J., 2014, 20, 2454-2458. (共同第一作者)

11、C. Bryan Huehls, Aijun Lin, Jiong Yang. “Iron-Catalyzed Intermolecular Hydroamination of Styrenes.” Org. Lett. 2014, 16, 3620-3623.

12、Zhi-Wei Zhang, Aijun Lin, Jiong Yang. “Methyl Ketone Oxime Esters as Nucleophilic Coupling Partners in Pd-Catalyzed C-H Alkylation and Application in the Synthesis of Isoquinolines”. J. Org. Chem., 2014, 79, 7041-7050.

13、Aijun Lin, Jiong Yang*, Mohamed Hashim. “N-Indolyltriethylborate: A useful reagent for synthesis of C3-quaternary indolenines.” Org. Lett., 2013, 15, 1950-1953,

14、Aijun Lin, Hao Peng, Ablimit Abdukader, Chengjian Zhu.* “Rhenium-Catalyzed Oxidative Cyanation of Tertiary Amines with TMSCN.” Eur. J. Org. Chem., 2013, 7286-7290.

15、Aijun Lin, Junying Wang, Haibin Mao, Yan Shi, Zhijie Mao, Chengjian Zhu.* “Organocatalytic Asymmetric Allylic Alkylation of Morita-Baylis-Hillman Carbonates with Phosphorus Ylides: Synthesis of Chiral 3-Substituted 2,4-Functionalized 1,4-Pentadienes.” Eur. J. Org. Chem., 2013, 6241-6245.

16、Haibin Mao, Aijun Lin, Yan Shi, Zhijie Mao, Xuebin Zhu, Weipeng Li, Hongwen Hu, Yixiang Cheng, Chengjian Zhu.* “Construction of Enantiomerically Enriched Diazo Compounds using Diazo Esters as Nucleophiles based on Chiral Lewis Base Catalysis.” Angew. Chem. Int. Ed., 2013, 52, 6288-6292.

17、Haibin Mao, Aijun Lin, Yang Tang, Yan Shi, Hongwen Hu, Yixiang Cheng, Chengjian Zhu.* “Organocatalytic oxa/aza-Michael-Michael Cascade Strategy for the Construction of Spiro Chroman/Tetrahydroquinoline-3,3’-oxindole Scaffolds.” Org. Lett., 2013, 15, 4062-4065.

18、Yan Shi, Aijun Lin, Haibin Mao, Zhijie Mao, Weipeng Li, Hongwen Hu, Chengjian Zhu*, Yixiang Cheng.* “Enantioselective Construction of Spirooxindole Derivatives through [3+2] Annulation Catalyzed by a Bisthiourea as a Multiple-Hydrogen-Bond Donor.” Chem. Eur. J., 2013, 19, 1914-1918.

19、Honglai Jiang, Aijun Lin, Chengjian Zhu*, Yixiang Cheng. “Copper-Catalyzed C-N Bond Formation through C-H/N-H Activation: A Novel Approach for the Synthesis of Multisubstituted Ureas.” Chem. Commun., 2013, 49, 819-821.

20、Hao Peng, Aijun Lin, Yan Zhang, Honglai Jiang, Jiecong Zhou, Yixiang Cheng, Chengjian Zhu*, Hongwen Hu. “Facile Oxidation and Amination of Benzylic sp3 C-H bond Catalyzed by Rhenium(V) Complexes.” ACS Catalysis, 2012, 2, 163-167.

21、Aijun Lin, Haibin Mao, Xi Zhu, Huiming Ge, Renxiang Tan, Chengjian Zhu*, Yixiang Cheng.* “Organocatalytic Enantioselective Amination of Morita-Baylis-Hillman Carbonates with Masked Ammonia: A Facile Method for the Synthesis of Unprotected a-Methylene-b-Amino Esters.” Chem. Eur. J., 2011, 17, 13676-13679.

22、Aijun Lin, Haibin Mao, Xi Zhu, Huiming Ge, Renxiang Tan, Chengjian Zhu*, Yixiang Cheng.* “Organocatalytic Asymmetric C-S bond Formation: Synthesis of a-Methylene-b-Mercapto Esters with Simple Alkyl Thiols”. Adv. Synth. Catal., 2011, 353, 3301-3306.

23、Aijun Lin, Junying Wang, Haibin Mao, Huiming Ge, Renxiang Tan, Chengjian Zhu*, Yixiang Cheng.* “Organocatalytic Asymmetric Michael-Type/Wittig Reaction of Phosphorus Ylides: Synthesis of Chiral a-Methylene-d-Ketoesters”. Org. Lett., 2011, 13, 4176-4179.

24、Aijun Lin, Ling Fang, Xi Zhu, Chengjian Zhu*, Yixiang Cheng.* “Organocatalytic Enantioselective Sulfenylation of β-Keto Phosphonates: A Convenient Approach to Construct Hetero-Quaternary Stereocenters”. Adv. Synth. Catal., 2011, 353, 545-549.

25、Xi Zhu, Aijun Lin, Ling Fang, Wei Li, Chengjian Zhu*, Yixiang Cheng.* “In Situ Formed Bifunctional Primary Amine–Imine Catalyst for Asymmetric Aldol Reactions of a-Keto Esters.” Chem. Eur. J., 2011, 17, 8281-8284.

26、Xi Zhu, Aijun Lin, Yan Shi, Jingyu Guo, Chengjian Zhu*, Yixiang Cheng.* “Enantioselective Synthesis of Polycyclic Coumarin Derivatives Catalyzed by an in Situ Formed Primary Amine-Imine Catalyst”. Org. Lett., 2011, 13, 4382-4385.

27、Ling Fang, Aijun Lin, Hongwen Hu, Chengjian Zhu*. “Highly Enantioselective Sulfenylation of b-Ketoesters: H-Bond Acceptor Catalysis”. Chem. Eur. J., 2009, 15, 7039-7043.