簡單介紹

1987年畢業于四川大學化學系,1992年于華西醫科大學太阳集团1088vip獲碩士學位,1997年于中國科學院化學研究所獲博士學位。1997-2000年在香港理工大學應用生物及化學科技系作博士後研究,2001-2003年在美國亞利桑納大學 (University of Arizona)化學系作訪問學者,2003年回國工作。現為中山大學藥物化學研究室教授,博士生導師,中山大學“百人計劃”引進人才,2006年入選教育部新世紀優秀人才,2011年入選“千百十工程”省級培養人才計劃。研究領域為不對稱合成反應、藥物合成新反應、手性藥物的合成工藝、新型抗菌藥物的設計、合成和篩選。先後主持國家自然科學基金項目、廣州市科技攻關項目、珠海市科技攻關項目、廣東省教育廳工程技術研究中心、中山大學啟動基金項目、教育部優秀人才項目。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.等國内外核心專業期刊上發表研究論文110餘篇,獲得國内外專利11項。

研究方向

1. 手性技術與不對稱合成反應
2. 新型抗菌藥物
3. 藥物的綠色合成工藝

教學情況

1.《藥物化學》 54學時
本課程講授化學小分子新藥的發明和研究方法、藥物的結構與活性的關系、結構修飾的技巧和藥物性質的調控方法、化學藥物的制備方法、常用藥物的物理化學性質、藥物分子與機體的相互作用。在新藥物的研究中,藥物化學處于整個研究鍊條的最前端,需要高度的創新能力, 涉及化學、生物學、生理學、細胞和分子生物學、免疫學等很多相關的學科知識。《藥物化學》是藥學專業本科生必修課程。
2.《手性藥物與不對稱合成》54 學時
本課程講授手性藥物的體内吸收、代謝、治療活性的差異和手性藥物的合成方法。重點介紹催化不對稱合成的基本思想、研究方法、各類最重要的反應類型、催化劑的設計和優化、國内外研究現狀。幫助學生了解不對稱合成方法在現代藥物、香料、農藥等工業中的應用價值,已取得的成就和面臨的問題,此外也啟發學生結合個人具體的研究課題産生新的想法和思路。本課程為有機化學和藥物化學方向的研究生選修課程。
 

科研項目

1.國家自然科學基金國際合作項目分項目

“靶向琥珀酸代謝的新抗菌藥物研究”(項目号:82061128001)

2021-2023, 50 萬元

2. 廣東省自然基金面上項目

乙烯基磺酰氟參與的不對稱加成反應研究 (項目号:2021A1515010503)

2021-2023,10 萬元

3. 國家自然科學基金項目

“烯基硫鎓鹽參與的不對稱串聯反應(項目号:21772240

2018-2021,64 萬元

4.國家自然科學基金項目

t-BuOK/DMF促進的自由基反應研究(項目号:21472248

2015-2018,85 萬元

5. 廣州市科技計劃項目

“有機催化法合成氨基丁酸類手性藥物研究” (項目号:201707010210

2017-202020萬元

6. 廣東省科技計劃項目

“抗前列腺增生藥物西洛多辛的合成新工藝研究”(項目号:2017A020211011

2017-2018,30萬元

7. 國家自然科學基金項目

基于α-硝基酮的有機催化串聯反應研究(項目号:21172270

2012-2015,60 萬元

 

論著專利

 近期發表論文:

  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 N2,2,2-Trifluoroethylisatin Ketimines to Ethylene Sulfonyl Fluoride, J. Org. Chem. 2021,86,30413048.

  7. Dong-yu Zhu, Xue-jing Zhang,* and Ming Yan,* Enantioselective Addition of Azlactones to Ethylene Sulfonyl Fluoride via Dual Catalysis, Org. Lett. 2021,23,42284232.

  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.

  

授權發明專利:

1. 鄢明、張天宇、張妞妞、劉志永、錢露、唐運祥、程亞娟、張學景,間二取代苯酚化合物及其制備方法與抗結核菌應用,中國發明專利201711310722.7

 

2.  鄢明、劉玉、張學景,一種合成右旋佐匹克隆的方法,中國發明專利201610408873.5

3.鄢明、董雪嬌、張學景, 一種合成氨基丁酸類手性化合物的方法,中國發明專利 201510053178.7

4.鄢明、王衛娟、張學景, 一種合成七元含氮雜環化合物的新方法,中國發明專利 201410134197.8

5.鄢明、孫翔,一種合成環狀脒類化合物的新方法,中國發明專利申請 201310270216.5

6.鄢明、陳豔豔、張學景,一種合成含氮雜環化合物的方法,中國發明專利 201310337282.X

7. 鄢明、位文濤、張學景、聶少振、陳豔豔,一種合成吲哚類化合物的方法,中國發明專利申請 201310337281.5

8. 鄢明、嚴雲雲、張學景,一種用于芳基烷烴氧化反應的催化體系及其應用,中國發明專利 201210479604.X

9. 鄢明、肖國強、殷霞,一種具有抗菌活性的3-硝基-2H-色烯類化合物及制備方法和用途,中國發明專利 201110031954.5

10. 鄢明,張學景,劉生平,手性磺胺類有機小分子催化劑及其應用,中國發明專利 200810027742.8

 

    專著:
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,陳新滋,"催化不對稱共轭加成反應新進展",(第17章,292-306 頁, 《不對稱有機反應》(李月明,範青華,陳新滋 主編),化學工業出版社,2005年1月第1版)。

   教材:

《藥物化學》,鄢明、成志毅 編著,科學出版社,2018