鄢明

鄢明

教授

研究领域:1. 手性技术与不对称合成反应
2. 新型抗菌药物
3. 药物的绿色合成工艺

办公电话: 020-39943049

联系邮箱: yanming@mail.sysu.edu.cn

简单介绍

1987年毕业于四川大学化学系,1992年于华西医科大学bm11222宝马娱乐网站获硕士学位,1997年于中国科学院化学研究所获博士学位。1997-2000年在香港理工大学应用生物及化学科技系作博士后研究,2001-2003年在美国亚利桑纳大学 (University of Arizona)化学系作访问学者,2003年回国工作。现为中山大学药物化学研究室教授,博士生导师,中山大学“百人计划”引进人才,2006年入选教育部新世纪优秀人才,2011年入选“千百十工程”省级培养人才计划。研究领域为不对称合成反应、药物合成新反应、手性药物的合成工艺、新型抗菌药物的设计、合成和筛选。先后主持国家自然科学基金项目、广州市科技攻关项目、珠海市科技攻关项目、广东省教育厅工程技术研究中心、中山大学启动基金项目、教育部优秀人才项目。至今已在J. Am. Chem. Soc.; Angew. Chem. Int. Ed.; Org. Lett.; J. Org. Chem; Chem.Commun.; Adv. Synth. Catal.; Org.Biomol.Chem.;Tetrahedron; Tetrahedron Lett.; Tetrahdron:Asymmetry.等国内外核心专业期刊上发表研究论文110余篇,获得国内外专利11项。

研究方向

1. 手性技术与不对称合成反应
2. 新型抗菌药物
3. 药物的绿色合成工艺

教学情况

1.《药物化学》 54学时
本课程讲授化学小分子新药的发明和研究方法、药物的结构与活性的关系、结构修饰的技巧和药物性质的调控方法、化学药物的制备方法、常用药物的物理化学性质、药物分子与机体的相互作用。在新药物的研究中,药物化学处于整个研究链条的最前端,需要高度的创新能力, 涉及化学、生物学、生理学、细胞和分子生物学、免疫学等很多相关的学科知识。《药物化学》是药学专业本科生必修课程。
2.《手性药物与不对称合成》54 学时
本课程讲授手性药物的体内吸收、代谢、治疗活性的差异和手性药物的合成方法。重点介绍催化不对称合成的基本思想、研究方法、各类最重要的反应类型、催化剂的设计和优化、国内外研究现状。帮助学生了解不对称合成方法在现代药物、香料、农药等工业中的应用价值,已取得的成就和面临的问题,此外也启发学生结合个人具体的研究课题产生新的想法和思路。本课程为有机化学和药物化学方向的研究生选修课程。
 

科研项目

1.国家自然科学基金国际合作项目分项目

“靶向琥珀酸代谢的新抗菌药物研究”(项目号:82061128001)

2021-2023, 50 万元

2. 广东省自然基金面上项目

乙烯基磺酰氟参与的不对称加成反应研究 (项目号:2021A1515010503)

2021-2023,10 万元

3. 国家自然科学基金项目

“烯基硫鎓盐参与的不对称串联反应”(项目号:21772240)

2018-2021,64 万元

4.国家自然科学基金项目

“t-BuOK/DMF促进的自由基反应研究”(项目号:21472248)

2015-2018,85 万元

5. 广州市科技计划项目

“有机催化法合成氨基丁酸类手性药物研究” (项目号:201707010210)

2017-2020,20万元

6. 广东省科技计划项目

“抗前列腺增生药物西洛多辛的合成新工艺研究”(项目号:2017A020211011)

2017-2018,30万元

7. 国家自然科学基金项目

“基于α-硝基酮的有机催化串联反应研究”(项目号:21172270)

2012-2015,60 万元

 

论著专利

 近期发表论文:

  1. Dong-yu Zhu, Yuan Chen, Xue-jing Zhang* and Ming Yan*,Regioselective conjugate addition of isoxazol-5-ones to ethenesulfonyl fluoride,Org. Biomol. Chem.2022,20,4714-4718.

  2. Peng Zhang, Jia Zeng, Ping Pan, Xue-jing Zhang, and Ming Yan*, Palladium-Catalyzed Migratory Insertion of Carbenes and C-C Cleavage of Cycloalkanecarboxamides,Org.Lett.2022,24,536-541.

  3. Lei Chen, Xiao-can Su, Rui-jun Peng, Xue-jing Zhang and Ming Yan*, Rh(III)-Catalyzed ortho C-H functionalization of aromatic amides with bis(phenylsulfonyl)diazomethane and α-diazosulfones,Org. Biomol. Chem.2022,20,3268-3272.

  4. Jie Chen, Yue Zhang, Dong-yu Zhu, Xue-jing Zhang* and Ming Yan*, Construction of Chiral Quaternary Carbon Stereocenters by Asymmetric Michael Addition of 4-Amido-5-hydroxylpyrazoles to Ethylene Sulfonyl Fluoride,Asian J.Org.Chem.2022,e202200063.

  5. Jing-xuan Zhou, Dong-yu Zhu, Jie Chen, Xue-jing Zhang,* Ming Yan,* and Albert S. C. Chan, Polysulfonate supported chiral diamine-nickel catalysts: Synthesis and applications, Tetrahedron Lett.2021,65,152792.

  6. Jie Chen, Dong-yu Zhu, Xue-jing Zhang,* and Ming Yan,* Highly Enantioselective Addition of N‑2,2,2-Trifluoroethylisatin Ketimines to Ethylene Sulfonyl Fluoride, J. Org. Chem. 2021,86,3041−3048.

  7. Dong-yu Zhu, Xue-jing Zhang,* and Ming Yan,* Enantioselective Addition of Azlactones to Ethylene Sulfonyl Fluoride via Dual Catalysis, Org. Lett. 2021,23,4228−4232.

  8. Bao-qin Huang, Yuan Chen, Xue-jing Zhang, and Ming Yan*, Cross-Dehydrogenative Coupling of Tetrahydroisoquinolines and 2-Fluoro-1,3-benzodithiole 1,1,3,3-tetraoxide: A New Synthetic Approach to α-Monofluoromethyl Tertiary Amines, Eur. J. Org. Chem. 2021,3015-3022

  9. Ping Pan, Lei Chen, Xue-jing Zhang, and Ming Yan*, Diverse functionalization of aryl halides mediated by bis(phenylsulfonyl)methane, Tetrahedron 2021,96, 132371.

  10. Lei Chen, Rui Jun Peng, Xue-jing Zhang, Ming Yan*, and Albert S. C. Chan, Aromatic C-H Methylation and Other Functionalizations via the Rh(III)-Catalyzed Migratory Insertion of Bis(phenylsulfonyl)carbene and Subsequent Transformations.J. Org. Chem.2021,86,10177-10189.

  11. Hua-ju Liang,Ya-juan Cheng,Lu-xia Wang,Bao-qin Huang,Niu-niu Zhang,Jie Liang,and Ming Yan*, Exploration of (3‐benzyl‐5-hydroxyphenyl) carbamates as new antibacterial agents against Gram‐positive bacteria, Arch. Pharm. Chem. Life Sci. 2020,353, e1900294.

  12. Zhen-Yu Chen,Bi-Zhen Lin,Lei Chen,Yong Zou,Ming Yan* and Xue-Jing Zhang*, Perfluorobutyl Iodide Mediated [1,2] and [2,3] Stevens Rearrangement for the Synthesis of Indolin-3-Ones, Adv. Synth. Catal. 2020,362,4368-437

  13. Jie Chen, Bao-qin Huang, Zeng-qing Wang, Xue-jing Zhang, and Ming Yan*, Asymmetric Conjugate Addition of Ethylene Sulfonyl Fluorides to 3‑Amido-2-oxindoles: Synthesis of Chiral Spirocyclic Oxindole Sultams, Org. Lett. 2019,21,9742-9746.

  14. Zhen-Yu Chen, Hua-Ju Liang, Ri-Xing Chen, Lei Chen, Xiang-Zheng Tang, Ming Yan* and Xue-Jing Zhang*, Cross-Dehygrogenative C-O Coupling of Oximes with Acetonitrile, Ketones and Esters, Adv. Synth. Catal. 2019,361,3324-3330.

  15. Ya-Juan Cheng, Zhi-Yong Liu, Hua-Ju Liang, Cui-Ting Fang, Niu-Niu Zhang, Tian-Yu Zhang,* and Ming Yan*, Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy, Molecules 2019,24,2021.

  16. Niu-niu Zhang, Bai-jiao An, Yan Zhou, Xing-shu Li* and Ming Yan *, Synthesis, Evaluation, and Mechanism Study of New Tepotinib Derivatives as Antiproliferative Agents, Molecules 2019,24,1173.

  17. Niu-niu Zhang, Yun-xiang Tang, Lu Qian, Ya-min Gao, Zhi-yong Liu, Zhi-liang Zou, Tian-yu Zhang*, Ming Yan*, Design, synthesis, and antitubercular activity of 3-amidophenols with 5-heteroatomic substitutions, Arch Pharm Chem Life Sci. 2019,352,e180027

  18. Xiang-Zheng Tang, Jie Liang, Xue-Jing Zhang, Raymond Wai-Yin Sun, Ming Yan*, Albert S. C. Chan, Synthesis of multisubstituted arylsulfones via a one-pot, three-component [3 + 3] benzannulation reaction, Org. Biomol. Chem. 2019,17, 4753-4760.

  19. Lei Chen, Jie Liang, Zhen-yu Chen, Jie Chen, Ming Yan*, Xue-jing Zhang*, A Convenient Synthesis of Sulfones via Light Promoted Coupling of Sodium Sulfinates and Aryl Halides, Adv. Synth. Catal. 2019,361,956-960.

  20. Shenquan Guo, Niuniu Zhang, Xiangzheng Tang, Zhifeng Mao, Xuejing Zhang, Ming Yan,* Yining Xuan*, Cyclopropanation of active methylene compounds withβ-alkoxycarbonyl vinylsulfonium salts, Chin. Chem. Lett. 2019,30,406-408.

  21. Lang Tong, Zhi-feng Mao, Xiang-zheng Tang, Xue-jing Zhang*, Ming Yan*, Cycloaddition of hydrazones and 1, 2-diarylalkynes promoted by t-BuOK/DMF: A convenient synthesis of tetraarylpyrazoles, Chin. Chem. Lett. 2019,30,395-397.

  22. Xiang-zheng Tang, Jing-xuan zhou, Hua-ju Liang, Xue-jing Zhang, Ming Yan*, Albert S. C. Chan,A practical synthesis of functionalized isoindolinones via [3 + 3] benzannulation of 1,3-bissulfonylpropenes and 4-arylmethylene-2,3-dioxopyrrolidines, Tetrahedron Lett. 2019,60, 147-149.

  23. Jie Liang, Yun-xiang Tang, Xiang-zheng Tang, Hua-jv Liang, Yamin Gao, Cuiting Fang, Tian-yu Zhang*, Ming Yan*, Discovery of meta-amido bromophenols as new antitubercular agents, Chem. Pharm. Bull. 2019,67,372-381.

  24. Zi-cong Chen, Lang Tong, Zhi-bo Du, Zhi-feng Mao,* Xue-jing Zhang, Yong Zou and Ming Yan*,Annulation of β-naphthols and 4-hydroxycoumarins with vinylsulfonium salts: synthesis of dihydrofuran derivatives, Org. Biomol. Chem.2018,16,2634-2638.

  25. Xiang-zheng Tang, Lang Tong, Hua-ju Liang, Jie Liang, Yong Zou, Xue-jing Zhang,* Ming Yan * and Albert S. C. Chan, Facile synthesis of substituted diaryl sulfones via a [3 + 3] benzannulation strategy, Org. Biomol. Chem.2018,16,3560-3563.

  26. Niu-niu Zhang, Zhi-yong Liu, Jie Liang, Yun-xiang Tang, Lu Qian, Ya-min Gao, Tian-yu Zhang * and Ming Yan *, Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents, Med. Chem. Commun. 2018,9,1293-1304.

  27. Zhen-yu Chen, Liang-yu Wu, Hai-sheng Fang, Ting Zhang, Zhi-feng Mao, Yong Zou, Xue-jing Zhang,* and Ming Yan,* Intramolecular hydroamidation of ortho-vinyl benzamides promoted by potassium tert-butoxide, Adv. Synth. Catal. 2017, 359, 3894-3899.

  28. Lin-Miao Ye, Lu Qian, Yan-Yan Chen, Xue-Jing Zhang and Ming Yan*,A practical synthesis of benzothiophenes via visible-light-promoted cyclization of disulfides and alkynes, Org. Biomol. Chem. 2017,15, 550-554.

  29. Ri-long Liu, Xiang-zheng Tang, Xue-jing Zhang, Ming Yan* and Albert S. C. Chan, Organocatalytic asymmetric conjugate addition of t-butyl nitroacetate to o-quinone methides: synthesis of optically active a-nitro-b,b-diaryl-propionates, RSC Adv. 2017, 7, 6660–6663.

  30. Lin-miao Ye, Jie Chen, Peng Mao, Zhi-feng Mao, Xue-jing Zhang, and Ming Yan**, Visible-light-promoted synthesis of benzothiazoles from 2-aminothiophenols and aldehydes, Tetrahedron Lett. 2017, 58, 874-876.

  31. Lin-miao Ye, Jie Chen, Peng Mao, Xue-jing Zhang, and Ming Yan*, Visible-light promoted synthesis of 3-arylthioindoles from indoles and diaryl disulfides, Tetrahedron Lett. 2017, 58, 2743-2746.

  32. Wang, Wei-juan; Chen, Jia-hua; Zhen, Zi-cong; Zeng, Yu-feng; Zhang, Xue-jing; Yan, M.; Chan, Albert S. C. A Convenient Synthesis of 1-Aryl- and 2-Aryl-Substituted Indazolones via Intramolecular C-N Coupling Promoted by KOt-Bu, Synthesis 2016, 48, 3551-3558.

  33. Yan-yan Chen, Zhen-yu Chen, Niu-niu Zhang, Jia-hua Chen, Xue-jing Zhang, Ming Yan*, Intramolecular Addition of Triarylmethanes to Alkynes Promoted by KOtBu/DMF: A Synthetic Approach to Indene Derivatives, Eur. J. Org. Chem. 2016, 3, 599-606.

  34. Chen, Jia-hua; Chen, Zi-cong; Zhao, Hong; Ting Zhang, Wei-juan Wang, Yong Zou, Xue-jing Zhang*, Ming Yan, Intramolecular addition of diarylmethanols to imines promoted by KOt-Bu/DMF: a new synthetic approach to indole derivatives, Org. Biomol. Chem. 2016, 14, 4071-4076.

  35. Jia-hua Chen, Zi-cong Chen, Hong Zhao, Yong Zou, Xue-jing Zhang* and Ming Yan*, Intramolecular cyclization of diarylmethanols to α,β-unsaturated amides promoted by KOt-Bu/DMF: a metal-free approach towards 3,4-disubstituted quinolinones, Org. Biomol. Chem. 2016, 11148-11153.

  

授权发明专利:

1. 鄢明、张天宇、张妞妞、刘志永、钱露、唐运祥、程亚娟、张学景,间二取代苯酚化合物及其制备方法与抗结核菌应用,中国发明专利201711310722.7

 

2.  鄢明、刘玉、张学景,一种合成右旋佐匹克隆的方法,中国发明专利201610408873.5

3.鄢明、董雪娇、张学景, 一种合成氨基丁酸类手性化合物的方法,中国发明专利 201510053178.7

4.鄢明、王卫娟、张学景, 一种合成七元含氮杂环化合物的新方法,中国发明专利 201410134197.8

5.鄢明、孙翔,一种合成环状脒类化合物的新方法,中国发明专利申请 201310270216.5

6.鄢明、陈艳艳、张学景,一种合成含氮杂环化合物的方法,中国发明专利 201310337282.X

7. 鄢明、位文涛、张学景、聂少振、陈艳艳,一种合成吲哚类化合物的方法,中国发明专利申请 201310337281.5

8. 鄢明、严云云、张学景,一种用于芳基烷烃氧化反应的催化体系及其应用,中国发明专利 201210479604.X

9. 鄢明、肖国强、殷霞,一种具有抗菌活性的3-硝基-2H-色烯类化合物及制备方法和用途,中国发明专利 201110031954.5

10. 鄢明,张学景,刘生平,手性磺胺类有机小分子催化剂及其应用,中国发明专利 200810027742.8

 

    专著:
1.Yue-Ming Li,Ming Yan, Albert S. C. Chan "Atropisomeric Partially Hydrogenated 1,1'-Binaphthyl Diphosphines"in Armin Borner Ed. "Phosphorus ligands in asymmetric cataltsis"pp (284-306),Wiley InterScience,2008.
2.鄢明,梁亮,陈新滋,"催化不对称共轭加成反应新进展",(第17章,292-306 页, 《不对称有机反应》(李月明,范青华,陈新滋 主编),化学工业出版社,2005年1月第1版)。

   教材:

《药物化学》,鄢明、成志毅 编著,科学出版社,2018