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冀亚飞

  

  

 


冀亚飞  教授 博士研究生导师 
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电话(传真): 021-64253314 
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通信地址:200237  上海市梅陇路130号363信箱

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E-mail:jyf@ecust.edu.cn
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个人简介
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1989年9月—1992年6月          华东化工学院精细化工系学习,获工学硕士学位。

1992年8月—1996年10月        安徽省药物研究所工作,任助理研究员。

1996年11月—2001年11月      中国矿业大学化工学院工作、学习,任讲师、副教授,获工学博士学位。

2001年12月—2003年11月      中国医学科学院中国协和医科大学药物研究所从事博士后科研工作。

2003年12月—2007年8月        华东理工大学药学院制药工程系从事制药工程和绿色化学领域的科研、教学工作,任副教授。

2007年9月                               评聘为教授。

2009年3月—2010年3月          赴美国University of New Mexico做访问学者

2011年4月—今                       制药工程系教授、博士研究生导师

    

       多年来国内外发表论文140余篇,获得中国发明专利授权10项,获省部级科技进步奖3项,上海市教学一等奖1项,校级奖项2项。担任制药工程系制药工艺学责任教授,受邀作为精细化工,应用化学,Research on Chemical Intermediates,Synthetic Communications, Catalysis Letters, Fuel Processing Technology国内外刊物审稿人;受邀作为国家自然科学基金委评议人。有多个药物合成工艺在企业得到应用,具有知识产权的新一代甲氧苄啶、甲乙基香兰素绿色技术居于领先水平。承担重大应用课题、国家自然科学基金、博士点基金等十余项科研课题。热情欢迎国内外企业合作开发化学药物及精细化工产品合成技术,热烈欢迎有志青年加盟从事制药工程与技术专业方向的硕士、博士学位研读,以及从事博士后研究。课题组同学多人获得国家博士、硕士研究生奖学金,及学校、学院研究生奖学金。

  

研究方向
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1 绿色化学 

2 杂环类药分子的设计与合成

3 药物制造过程的绿色工艺

4 有机合成中的区域与立体选择性控制研究 

 

获奖成果
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20174月主持“制药工艺学”上海市精品课程建设

2017年4月获2016年华东理工大学教学成果一等奖深化制药工艺学课程建设,践行“卓越工程师培养计划”素质教育

20149月获2013年高等教育上海市教学成果一等奖:强实践、重创新,培养适应现代制药工程需求的专业人才

2014年1月获华东理工大学2013年度研究生课程优秀任课教师一等奖

2011年9月华东理工大学国家技术转移中心:“优秀技术转移项目” 

2008年9月华东理工大学教育教学成果一等奖:“制药工程专业质量保障体系”

2006年12月获江苏省科技进步奖三等奖:“煤的高效利用研究”

2006年11月获中国石油和化学工业科技进步奖一等奖:“煤的高附加值利用的基础研究”

2004年11月获山东省科技进步奖三等奖:“甲氧苄啶的研制与开发”

  

代表性论文
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Fu XP, Tang SB, Yang JY, Zhang LL, Xia CC, Ji YF.* Cascade reaction to synthesis of carbolines from O-methylketoximes and styrenes via palladium-catalyzed C–H bond activation and sequential annulation. Eur. J. Org. Chem. 2019-7-19, Published online, DOI: 10.1002/ejoc.201901035.

 

Deng KZ, Zhang LL, Chen YF, Xie HX, Xu XB, Xia CC, Ji YF.* Copper-mediated direct thiolation of aryl C–H bonds with disulfides. Org. Biomo. Chem. 2019-7-23, Published online, DOI: 10.1039/c9ob01255a.

 

Yang JY, Fu XP, Tang SB, Deng KZ, Zhang LL, Yang XJ, Ji YF.* 2-Amino-5,6- difluorophenyl-1H-pyrazole-directed Pd(II) catalysis: arylation of unactivated C(sp3)-H bonds. J. Org. Chem. 2019-7-22, Published online, DOI: 10.1021/acs.joc.9b01276. 


Xing LH, Shao LY, Fu XP, Deng KZ, Yang JY, Ji YF.* Palladium-catalyzed thiazole-directed mono-selective C(sp2)-H bond iodination reaction. Chin. J. Org. Chem. 2019, 39, Published online, DOI: 10.6023/cjoc201904062. 


Fu XP, Yang JY, Deng KZ, Shao LY, Xia CC,* Ji YF.* Tandem C–C/C–N formation via palladium-catalyzed C–H activation/styrenation and sequential annulation of O-methylketoxime with styrenes. Org. Lett. 2019, 21, 3505–3509.

  

Chen MM, Shao LY, Lun LJ, Wu YL, Fu XP, Ji YF.* Palladium-catalyzed late-stage mono-aroylation of the fully substituted pyrazoles via aromatic C–H bond activation.Chin. Chem. Lett. 2019, 30, 702706. 

  

Shao LY, Wang CY,* Fu XP, Chen XX, Liu HW, Ji YF.* Palladium-catalyzed direct mono-aroylation of O-arylmethyl and aryl substituted acetoxime ethers. Org. Biomol. Chem. 2018, 16, 6284–6294.    

  

Hu YH, Shao LY, Ji YF.* Palladium-catalyzed arylation of aromatic amides directed by 2-amino-5-cholophenyl-1H-pyrazole auxiliary. Synlett 2018, 29, 1875–1880.  


Shao LY, Xing LH, Guo Y, Yu KK, Wang W, Liu HW, Liao DH, Ji YF.* Catalytic cascade access to biaryl-2-methyl acetates from pyruvate O-arylmethyl ketoximes via the palladium-catalyzed C(sp2)–H bond arylation and C–O bond solvolysis. Adv. Synth. Catal. 2018,360, 2925–2937.


Qiao WL,Shao LY, Hu YH, Xing LH, Deng KZ, Liao DH, Dao-Hua Liao, Ji YF.* Palladium-catalyzed Csp3–H bond mono-aroyloxylation of O-alkyl substituted 2,4,6-trimethoxybenzaldoximeethers. Synlett 2018, 29, 1249–1255.


Guo Y, Shao LY, Yu KK, Hu YH, Liu HW,* Liao DH, Ji YF.* Palladium-catalyzed site-selective direct olefination of 6-electron-withdrawing group substitued 3-arylbenzo[d]isoxazoles. Org. Chem. Front. 2017, 4, 19621966.


Guo Y, Yu KK,Xing LH, Liu HW, WangW,* Ji YF.* Palladium-catalyzed divergent regioselective homocoupling and hydroxylation of 3-arylbenzo[d]isoxazoles. Adv. Synth. Catal. 2017, 359(3), 410418.


Shao LY, Li C, Guo Y, Yu KK, Zhao FY, Qiao WL, Liu HW, Liao DH, Ji YF*. Pd-catalyzed direct oxidative mono-aroyloxylation ofO-aralkyl substituted acetoxime ethers. RSC Advances, 2016, 6, 7887578880. 


Yu, KK, Guo Y, Hu YH, Xu Z, Liu HW, Liao DH, Ji YF*. Pd-catalyzed diverse mono-acyloxylation of 5-alkyl-4-aryl-thiazole-2-carboxylates. Asian J. Org. Chem. 2016, 5, 219–1224.


Ding J, Guo Y, Shao LY, Zhao FY, Liao DH, Liu HW*, Ji YF*. Palladium-catalyzed multi-acetoxylation of 1,3-disubstituted 1H-pyrazole-5-carboxylatesvia direct C(sp2)−H or C(sp3)−H bond activation. Chin. Chem. Lett. 2016, 27, 1617–1621.


Fan XM, Guo Y, Li YD,Yu KK, Liu HW, Liao DH, Ji YF*. Pd-catalyzed late-stage mono-acetoxylation and mono-iodination of 4-alkyl-1,5-diaryl-1H-pyrazole-3-carboxylates via direct Csp2-H bond activation. Asian J. Org. Chem. 2016, 5, 499–505. 


Zhang ZN, Huang JG, Zhai JJ, Guo Y, Ji YF*. Copper(II)-catalyzed oxidative esterification of substituted p-cresols under ligand- and additive-free conditions. Synlett 2015, 26, 2145–2150. 


Guo Y, Li YD, Chen C, Zhao JH, Liu HW, Liao DH, Ji YF*. A practical ligand-free copper(I) bromide-catalyzed fluoroalkoxylation of unactivated aryl bromides. Res. Chem. Intermediat. 201642, 2525–2537. 


Huang JG, Guo Y, Li YD, Liu HW,* Liao DH, Ji YF*. Undecorated Cu(OAc)2-catalyzed C(sp3)–C(sp3) bond formation through a para-hydroxyl group-triggered remote benzylic C(sp3)–H bond functionalization. Eur. J. Org. Chem. 2015, 5334–5338.   


Guo Y, Fan XM, Nie M, Liu HW, Liao DH, Pan XD,* Ji YF*. Practical ligand-free Cu-catalyzed short-chain alkoxylation of unactivated aryl bromides. Eur. J. Org. Chem2015, 47444755.


Guo Y, Chen C, Liu HW,* Zhao JH, Zheng, YL, Ji YF*. A ligand-free, powerful and practical method for methoxylation of unactivated aryl bromides by use of CuCl/HCOOMe/MeONa/MeOH system. Res. Chem. Intermediat. 2015, 41, 8651–8664.


Zhai JJ, Gu CH, Guo Y, Liao DH, Zhu DR, Ji YF*. One-pot synthesis of highly substituted 1H-pyrazole-5-carboxylates from 4-aryl-2,4-diketoesters and arylhydrazines. J. Heterocyclic Chem. 2016, 53, 840–848.


Huang JG, Guo Y, Jiang JA, Liu HW, Ji YF*. An eco-friendly Co(OAc)2-catalyzed aerobic oxidation of 4-benzylphenols into 4-hydroxybenzophenones. Res. Chem. Intermediat. 2015, 41, 7115–7124.


Jiang JA, Chen C, Guo Y, Liao DH, Pan XD, Ji YF*. A highly efficient approach to vanillin starting from 4-cresol. Green Chem. 2014,16, 2807–2814. 


Gu CH, Zhai JJ, Jiang JA, Liu HW, Wang L, Zhu DR, Ji YF*. An efficient one-pot synthesis of aryl-substituted 1-(thiazol-2-yl)-1H-pyrazole-3-carboxylates via a Hantzsch synthesis-Knorr reaction sequence. Chin. J. Chem. 2014, 32, 179–190. 


Jiang JA, Chen C, Huang JG, Liu HW, Cao S, Ji YF*. Cu(OAc)2-catalyzed remote benzylic C(sp3)–H oxyfunctionalization for C=O formation directed by the hindered para-hydroxyl group with ambient air as terminal oxidant under ligand- and additive-free conditions. Green Chem. 2014, 16, 1248–1254.  


Jiang JA, Du JL, Liao DH, Wang ZG, Ji YF*. Efficient Co(OAc)2-catalyzed aerobic oxidation of EWG-substituted 4-cresols to access 4-hydroxybenzaldehydes. Tetrahedron Lett. 2014,5 5, 1406–1411.  


Zhai  JJ, Gu CH, Jiang JA, Zhang SL, Liao DH, Wang L, Zhu DR, Ji YF*. A one- pot approach to ethyl 1,4,5-triaryl-1H-pyrazole-3-carboxylates via an improved Claisen condensation-Knorr reaction sequence. Chin. J. Chem. 2013,31, 1526–1538.   


Jiang JA, Du JL, Zhang ZN, Zhai JJ, Ji YF*. An environmentally friendly and highly efficient Co(OAc)2-catalyzed aerobic oxidation to access 2,6-di-electron-donating group substituted 4-hydroxybenzaldehydes. Syn. Commun2014,44, 1430–1440.      


Zhai JJ, Jiang JA, Zhang SL, Chen C, Liu HW, Liao DW, Ji YF*. Stereoselective or exclusive synthesis of ethylZ-2-(2-substituted-thiazol-4-yl)pent-2-enoates from ethylE/Z-2-(2-bromoacetyl)pent-2-enoate. Synlett 2013, 24, 1399–1404.   

  

Huang WB, Guo Y, Jiang JA, Pan XD, Liao DH, Ji YF*. An efficient strategy for protecting dihydroxyl groups of catechols. Synlett 2013,24, 741–746.


Jiang JA, Huang WB, Zhai JJ, Liu HW, Cai Q, Xu LX, Wang W, Ji YF*. “One-pot” synthesis of 4-substituted 1,5-diaryl-1H-pyrazole-3-carboxylates via lithiumtert-butoxide-mediated sterically hindered Claisen condensation and Knorr reaction. Tetrahedron 2013, 69, 627635.


Jiang JA, Ji YF*.  Alternative synthesis of apixaban (BMS-562247), an inhibitor of blood coagulation factor Xa.Syn. Commun. 2013, 43, 72–79.


Jiang JA, Du CY, Gu CH, Ji YF*. “One-pot” synthesis of 4-substituted 1,5-diaryl-1H-pyrazole-3- carboxylic acids via a MeONa/LiCl-mediated sterically hindered Claisen condensation-Knorr reaction-hydrolysis sequence. Synlett 2012, 23, 2965–2968.   


Huang WB, Du CY, Jiang JA, Ji YF*. Concurrent synthesis of vanillin and isovanillin. Res. Chem. Intermediat. 2013, 39, 2849–2856. 


Ji YF*, Jiang JA, Liu HW, Liao DH, Wei XY. Practical preparation of trimethoprim: a classical antibacterial agent. Syn. Commun. 2013, 43, 1517–1522.




 

授权专利

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卫洁,刘倩,丁涛,王树华,冀亚飞.一种制备质子泵抑制剂硫醚中间体的方法.中国发明授权专利号:ZL2012102112430,申请日:2012-06-26.

冀亚飞,张鹏志,万欢,段梅莉,许煦,王毅. 一种5-(4-氯苯基)-1-(2,4二氯苯基)-4-甲基吡唑-3-甲酸酯的制备方法. 中国发明授权专利号:ZL200810038071.5,申请日:2008-05-23.

段梅莉,辛秀娟,鲍杰,冀亚飞,英智威,李慧. 一种脱氧核苷三磷酸的分离提纯方法. 中国发明授权专利号:ZL200810040986.X,申请日:2008-07-25.

冀亚飞,金文虎,万欢,段梅莉. 一种芳香族甲醚化合物的制备方法. 中国发明授权专利号:ZL200810036967.X,申请日:2008-05-05.

冀亚飞,万欢,方峰,段梅莉,许煦. 一种3-苄胺基-2-(3,4,5-三甲氧基苄基)丙烯腈的制备方法. 中国发明授权专利号:ZL200810036968.X,申请日:2008-05-05.

冀亚飞,江健安,刘倩,禹艳坤,王超,刘爱霞,王毅. 抗血栓药物阿匹沙班(Apixaban,BMS-562247)的制备方法. 中国发明授权专利号:ZL201010277358.0,申请日:2010-09-10.

冀亚飞,王超,禹艳坤,刘倩,江健安,刘爱霞,王毅. 一种制备祛痰药物氨溴索关键中间体反式-4-[(2-氨基苄基)氨基]-环己醇方法. 中国发明授权专利号:ZL201010567715.7,申请日:2010-11-29.

冀亚飞,禹艳坤,江健安. 一种抗肿瘤药物伊马替尼的制备方法. 中国发明授权专利号:ZL201010589207.9,申请日:2010-12-15.

冀亚飞,万欢,臧佳良,陈一芬,金文虎,王毅. 一种制备香兰素及其类似物的方法.中国发明授权专利号:ZL200910045117.0,申请日:2009-01-09  

冀亚飞,翟娇娇,江健安,黄伟彬,杜彩彦,王毅. 一种制备顺式-2-(2-叔丁氧甲酰胺基噻唑-4-基)-2-戊烯酸的方法. 中国发明专利申请号:ZL201210005520.2 申请日:2012-01-09.

冀亚飞,黄伟彬,江健安,翟娇娇. 一种并发合成香兰素和异香兰素的方法. 中国发明专利申请号:201210069087.9 申请日:2012-03-15.

  

著作

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译著:施小新,冀亚飞,邓卫平译.《工业规模的不对称催化(第1版)》,上海:华东理工大学出版社2006.冀亚飞参与翻译10万字的内容.

参编教材:赵临襄主编,《化学制药工艺学(第4版)》,北京:中国医药科技出版社,2015-09-01出版.出版书号:ISBN 978-7-5067-7423-9.冀亚飞编写《甲氧苄啶的生产工艺原理》一章,约5万字。

 

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