胡跃飞 教授


清华大学化学系,北京 100084

email:yfh@mail.tsinghua.edu.cn

电话:010-62795380

教育背景

1988-1990 美国南佛罗里达大学《分子设计和识别中心》,G. R. Newkome 教授课题组 博士后

1984-1987 南京大学化学系 理学博士

1980-1983 南京大学化学系 理学硕士

1977-1980 南京大学化学系 大学毕业

工作履历

2002-至 今 清华大学化学系教授,博士生导师。

1996-2002 南京大学化学系教授,博士生导师。

1991-1996 美国华盛顿大学医学院 (St. Louis) 分子生物学和分子药理学系工作,Research Associate,D. F. Covey 教授课题组。

1987-1988 南京大学化学系讲师。

1983-1984 北京理工大学助教。

学术兼职

中国化学会《化学学报》编委会委员 (1999- )

中国化学会《化学化学生物学专业委员会》委员 (2001- )

社会兼职

中国化学会会员 (1997- )

研究领域

生物有机化学 具有生物活性的复杂和天然化合物的设计、合成和性质研究

杂环化学 具有生物活性杂环化合物的合成和方法研究

不对称合成 手性化合物的合成和方法研究

药物化学 国家级新药的研制

奖励与荣誉

1998年 教育部“跨世纪人才培养计划基金”获得者。

2000年 国家基金委“国家杰出青年基金” 获得者。

2000年 中国化学会首届“有机合成杰出青年奖” 获得者

学术成果

已经发表的部分论文

Yanmei Dong, Rui Li, Jun Lu, Xuenong Xu, Xinyan Wang, Yuefei Hu*, An efficient kinetic resolution of racemic Betti base based on an enantioselective N,O-deketalization. J. Org. Chem., 2005, 70, 8617-8620. Cunde Wang, Xin Jiang, Haijian Shi, Jun Lu, Yuefei Hu* and Hongwen Hu, Optimization of the abnormal Beckmann rearrangement: Application to steroid 17-oximes. J. Org. Chem., 2003, 68, 4579-4581.

Rui Zhu, Lixin Xing, Xinyan Wang, Chuanjie Cheng, Bo Liu and Yuefei Hu*, Practical preparation of diosphenols by ring-opening of epoxyketones catalyzed by silica gel supported acids, Synlett 2007, 2267-2271.

Lixin Xing, Xinyan Wang, Chuanjie Cheng, Rui Zhu, Bo Liu and Yuefei Hu*, A solvent-controlled highly efficient Pd-C catalyzed hydrogenolysis of benzaldehydes to methylbenzenes via a novel “acetal pathway”, Tetrahedron2007, 63, 9382-9386.

Liya Cao, Jianwei Sun, Xinyan Wang, Rui Zhu, Haijian Shi, Yuefei Hu*, Total synthesis of (-)-elegansidiol by using an abnormal Beckmann rearrangement of Hajos ketone oxime as a key step, Tetrahedron 2007, 63, 5036-5041.

Chuanjie Cheng, Xinyan Wang, Lixin Xing, Bo Liu, Rui Zhu and Yuefei Hu*, An efficient and practical method for highly chemoselective hydrogenation of nitrobenzylaminesto aminobenzylamine hydrochlorid, Adv. Synth. Catal., 2007, 349, 1775-1780.

Yuefei Hu, Hua Fu, Chanjuan Xi and Yong Ju, Reagents for Modern Organic Synthesis—Properties, Preparations and Reactions (Book), Chemical Industry Publisher: Beijing 2006, 443 pp, Hardback, ISBN 7-5025-8542-7.

Shaozhong Wang,* Jia Pan, Yuefei Hu, Hongwen Hu, FeCl3-promoted intramolecular annulation of δ-keto nitriles:Facile approach to prepare 3-acetamido-2-pyridone derivatives. Synthesis 2005, 753-756.

Shaozhong Wang,Yanmei Dong, Xinyan Wang, Xiaoyi Hu, Jun O Liuand Yuefei Hu*, 3-Aryl-β-carbolin-1-ones as inhibitors fortumor cell proliferation: Synthesis and biological evaluation. Org. Biomol. Chem., 2005,3,911-916.

Xinyan Wang, Yanmei Dong, Jianwei Sun, Rui Li, Xuenong Xu and Yuefei Hu*, Nonracemic Betti base as a new chiral auxiliary: Application to total syntheses of enantiopure (2S,6R)-dihydropinidine and (2S,6R)-isosolenopsins. J. Org. Chem., 2005, 70, 1897-1900.

Shaozhong Wang, Liya Cao, Haijian Shi, Yanmei Dong, Jianwei Sun and Yuefei Hu*, Preparation of 2-pyridone-containing tricyclic alkaloid derivatives as potential inhibitors of tumor cell proliferation by regioselective intramolecular N- and C-acylation of 2-pyridone. Chem. Pharm. Bull., 2005, 53, 67-71.

Jianwei Sun, Yanmei Dong, Liya Cao, Xinyan Wang, Shaozhong Wang and Yuefei Hu*, Highly efficient chemoselective deprotection of O,O-acetals and O,O-ketals catalyzed by molecular iodine in acetone, J. Org. Chem., 2004, 69, 8932-8934.

Shaozhong Wang,Jianwei Sun,Gang Yu,Xiaoyi Hu,Jun O Liuand Yuefei Hu*, CuI catalyzed N-arylation of amide as a key step for the preparation of 3-aryl β-carbolin-1-ones, Org. Biomol. Chem., 2004, 1573-1574.

Yanmei Dong, Jianwei Sun, Xinyan Wang, Xuenong Xu, Liya Cao and Yuefei Hu*, Highly regioselective N-alky-lation of non-racemic Betti base: A novel one-pot synthesis of chiral N-methyl-N-alkyl Betti bases. Tetrahedron: Asymmetry 2004, 15, 1667-1672.

Gang Yu, Shaozhong Wang, Kai Wang Yuefei Hu* and Hongwen Hu, A novel approach to 1,2-dihydro-2-oxo-3-pyridinecarboxylic ester via aromatization induced by deamidation. Synthesis 2004, 1021-1028.

Xuenong Xu, Jun Lu, Yanmei Dong, Rui Li, Zongming Ge and Yuefei Hu*, An improved synthesis of chiral 1-[α-(1-azacycloalkyl)benzyl]-2-naphthols. Tetrahedron: Asymmetry 2004, 15, 475-479.

Xuenong Xu, Jun Lu, Rui Li, Zongming Ge, Yanmei Dong and Yuefei Hu*, Diastereopure preparation of α-benzotriazolyl 1-azacycloalka[2,1-b][1,3] oxazines and their application as versatile chiral precursors, Synlett2004, 122-124.

Shaozhong Wang, Gang Yu, Jun Lu, Kun Xiao, Yuefei Hu* and Hongwen Hu, A novel and regioselective tandem reaction between 2-acetamidoacetamide and chalcones promoted by Cs2CO3 for the preparation of 3-unsubstituted 4,6- diarylpyrid-2-ones. Synthesis 2003, 487-490.

Jun Lu, Xuenong Xu, Shaozhong Wang, Cunde Wang, Yuefei Hu* and Hongwen Hu, Novel preparation of non-racemic 1-[a-(1-azacycloalkyl)benzyl]-2-naphthols from Betti base and their application as chiral ligands in the asymmetric addition of diethylzinc to aryl aldehydes, J. Chem. Soc., Perkin Trans 1., 2002, 2900-2903.

Jun Lu, Xuenong Xu, Cunde Wang, Jiangang He, Yuefei Hu* and Hongwen Hu, Synthesis of chiral ligands derived from the Betti base and their use in the enantioselective addition of diethylzinc to aromatic aldehydes, Tetrahedron Lett., 2002, 43, 8367-8369.

Jie Wang,Xin Jiang, Ming Chen, Zongming Ge, Yuefei Hu* and Hongwen Hu, TFA catalyzed ring transformation of 4-hydroxycyclobutenone: TFA catalyzed ring transformation of 4-hydroxycyclobutenone: A facile and general route for preparation of 3-substituted 4-amino-2(5H)-furanones. J. Chem. Soc., Perkin Trans 1., 2001, 66-71.

Xin Jiang, Jie Wang, Jiaxin Hu, Zongming Ge, Yuefei Hu* and Hongwen Hu, Synthesis of (5a)-17-azaandrostan-3-ols and (5a)-17-aza-D-homoandrostan-3-ols and their N-acylated derivatives. Steroids 2001, 66, 655-662.

Jie Wang,Xin Jiang, Ming Chen, Yuefei Hu* and Hongwen Hu, A novel coupling reaction of cyclobutene-1,2-diones induced by low-valent titanium. J. Organomet. Chem., 2001, 629, 213-218.

Jiaxin Hu, Xin Jiang, Ting He, Jan Zhou, Yuefei Hu* and Hongwen Hu, Novel synthetic routes for nitrogen-bridged tricyclic derivatives of pyrrolo[2,1,5-cd] indolizine and pyrrolo[2,1,5-de]quinolizine derived from 2-acyl-N-(acylmethyl- ene)pyridinium halides. J. Chem. Soc., Perkin Trans 1., 2001, 1820-1825.

Feng Liang, Jiaxin Hu, Lande Zhang, Yuefei Hu* and Hongwen Hu, Preparation of pyrrolo[2,1,5-cd]indolizine derivatives by intramolecular condensation of 3-acyl-5-methylindolizines. J. Heterocyclic Chem., 2001, 38, 853-857.

Xin Jiang, Cunde Wang, Yuefei Hu* and Hongwen Hu, A practical and facile route for the preparation of 18-norandrostan-17-ones from androstan-17-ones using SmI2 promoted cyclization and dehydroxylation. J. Org. Chem., 2000, 65, 3555-3557.

D.F. Covey,*M. Han, A.S. Kumar, M.A.M. de la Cruz, E.S. Meadows,Yuefei Hu, A. Tonnies, D. Nathan, M. Coleman, A. Benz, A.S. Evers, C.F. Zorumski, S. Mennerick, Neurosteroid analogues. 8. Structure-activity studies of N-acylated 17a-aza-D-homosteroid analogues of the anesthetic steroids (3a,5a)- and (3a,5b)-3-hydroxypregnan-20-one. J. Med. Chem., 2000, 43, 3201-3204.

Lande Zhang,Feng Liang, Lingzhi Sun, Yuefei Hu* and Hongwen Hu, A novel synthesis of 3-unsubstituted indolizines. Synthesis 2000, 1733-1737.

Jian Zhou,Yuefei Hu* and Hongwen Hu, Synthesis of pyrrolo[2,1-a]phthalazines by 1,3-dipolar cycloaddition of phthalazinium N-ylides with alkenes in the presence of tetrakis-pyridine cobalt (II) dichromate. J. Heterocyclic Chem.,2000, 37, 1165-1168.

Bingxiang Wang, Jiaxin Hu, Xuechun Zhang, Yuefei Hu* and Hongwen Hu, Oxidant promoted 1,3-dipolar cycloaddition of benzimidazolium ylides to alkenes for preparation of 4H-pyrrolo[1,2-a]benzimidazole. J. Heterocyclic Chem., 2000, 37, 1533-1537.

Bingxiang Wang, Xuechun Zhang, Jun Li, Xin Jiang, Yuefei Hu* and Hongwen Hu, Preparation of 3-indolizincarboxamides and 3-indolizinecarbonitriles by 1,3-cycloaddition of N-cyanomethylpyridinium ylides with alkenes in the presence of TPCD or MnO2. J. Chem. Soc., Perkin Trans I, 1999, 1571-1575.

Jian Zhou, Yuefei Hu,* Hongwen Hu, The first approach to the synthesis of indolizines by intramolecular 1,5-dipolar cyclization of 2-(2-arylethenyl)pyridium ylides in the presence of tetrakis-pyridine cobalt (II) dichromate. Synthesis 1999, 166-170.

Yuefei Hu, L.L. Wittmer, M. Kalkbrenner, A.S. Evers, C.F. Zorumski, D.F. Covey*, Neurosteroid analogues 5. Enantiomers of neuroactive steroids and benz[e]indenes: total synthesis, electrophysiological effects on GABAA receptor function and anesthetic action in tadpoles. J. Chem. Soc., Perkin Trans I, 1997, 3665-3671.

Yuefei Hu, K.A. Yamada, D.K. Chalmers, D.P. Annavajjula, D.F. Covey*, Enantioselectivity synthesis of cyclothiazide analogues: Novel probes of the stereospecific actions of benzothiadizines at AMPA-type glutamate receptors. J. Am. Chem. Soc., 1996, 118, 4550-4559.

L.L. Wittmer, Yuefei Hu, M. Kalkbrenner, A.S. Evers, C.F. Zorumski, D.F. Covey*, Enantioselectivity of steroid-induced GABAA receptor modulation and anesthesia. Molecular Pharmacology 1996, 50, 1581-1586.

Yuefei Hu, C.F. Zorumski, D.F. Covey*, Neurosteroid analogues. 2. Total synthesis and electrophysiological evaluation of a benz[e]indene analogue of the anesthetic steroid alphaxalone. J. Org. Chem., 1995, 60, 3619-2635.

Yuefei Hu, P.C. Sherwin, D.F. Covey*, Synthesis of (17R)- and (17S)-hydroxy-14,15-secoandrost-4-en-15-yn-3-one and the X-ray structure of the (17S)-diastereomer. Steroids, 1995, 60, 491-496.

M. Han, Yuefei Hu, C.F. Zorumski, D.F. Covey*, Neurosteroid analogues. 3. Synthesis and electrophysiological evaluation of benz[e]indene congeners of neuroactive steroids having the 5b-cofiguation. J. Med. Chem., 1995, 38, 4548-4556.

Yuefei Hu,* Xudong Wei, Hongwen Hu, Tetrakis-pyridino-cobalt (II) dichromate Py4Co(HCrO4)2 (TPCD). in Encyclopedia of Reagents for Organic Synthesis, Ed. by L.A., Paquette, John Wiley & Sons, New York, 1995, Vol. 7, 4780-4781.

B.P. Schlegel, J.E. Pawlowski, Yuefei Hu, D.M. Scolnick, D.F. Covey, T.M. Penning*, Steroid mechanism-based inactivators and site-directed mutagenesis as probes for steroid hormone recognition by 3a-hydroxysteroid dehydrogenase. Biochemistry, 1994, 33, 10367-10374.

Yuefei Hu, D.F. Covey*, Synthesis of 1,10-seco-5a-estr-1-ynes: Potential mechanism-based inhibitors of 3a- and 3b-hydroxysteroid dehydrogenases. J. Chem. Soc., Perkin Trans. I, 1993, 417-422.

Xudong Wei, Yuefei Hu*, Tingshen Li, Hongwen Hu, A facile one-step synthesis of aromatic indollizines by 1,3-dipolar cycloaddition of pyridinium and related heteroaromatic ylides with alkenes in the presence of TPCD [Py4Co(HCrO4)2]. J. Chem. Soc., Perkin Trans. I, 1993, 2487-2489.

Yuefei Hu, C.F. Zorumski, D.F. Covey*, Structure-activity studies of ben[e]indenes modulation of GABA reception function. 1. The effect of 6-methyl substituted on electrophisiology activity. J. Med. Chem., 1993, 36, 3956-3967.

D.F. Covey*, Yuefei Hu, M.G. Bouly, K.D. Holland, N.T. Rodgers-Neame, K.E. Isenberg, C.F. Zorumski, Modulation of GABA receptor function by benz[e]indenes and phenanthrenes. J. Med. Chem., 1993, 36, 627-630.

已申请和批准的专利

胡跃飞,许学农,李锐,董艳梅,陆军,胡宏纹,1-(a-氨基苄基)-2-萘酚的缩酮 (醛) 化合物及其制法和用途,中国发明专利,申请号: 02157261.5,受理日期:2002.12.26。

胡跃飞,陆军,许学农,王少仲,胡宏纹,手性化合物 S-(+)- 和 R-(-)- 1-(a-氨基苄基)-2-萘酚的制备方法,中国发明专利,申请号:01129170.1,受理日期:2001.09.04。公开日期:2002.05.15。

D.F. Covey, Yuefei Hu, C.F. Zorumski. Novel Tricyclic Steroid Analogs. European Patent. Patent No. 0548824. Patent data: Jan. 31, 1996.

D.F. Covey, Yuefei Hu, M. Han, C.F. Zorumski, Benz[e]indene Compounds. United States Patent, Patent No. 5,434,274. Patent data: July 18, 1995. Int. Cl. C07D 317/72. U.S.Cl. 549/336.

D.F. Covey, Yuefei Hu, C.F. Zorumski, Tricyclic Steroid Analogs. United States Patent, Patent No. 5,292,906. Patent data: March 08, 1994. Int. Cl. C07C 69/74. U.S.Cl. 552/619.

D.F. Covey, Yuefei Hu, C.F. Zorumski, Tricyclic Steroid Analogs. United States Patent, Patent No. 5,344,826. Patent data: Sept. 06, 1994. Int. Cl. A01N 45/00. U.S.Cl. 514/167.

D.F. Covey, Yuefei Hu, C.F. Zorumski. Tricyclic Steroid Analogs. United States Patent, Patent No. 5,206,415. Patent data: April 27, 1993. Int. Cl. C07C 69/608. U.S.Cl. 560/117.