冀亚飞-全讯国际

冀亚飞  教授 博士研究生导师 
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微信号留言: ecust-jyf 

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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:
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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170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6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等国内外刊物的审稿人；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

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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2021年12月获2020-2021学年度：华东理工大学优秀研究生指导教师

2021年6月获2020年华东理工大学教学成果二等奖：线上线下一体化的《制药工艺学》课程建设与实践

2020年12月荣获2020年度华东理工大学“东岳药业研究生奖教金”

2019年12月获2018年华东理工大学教学成果二等奖：上海市精品课程《制药工艺学》课程建设与实践

2017年4月主持“制药工艺学”核心课程被授予上海市精品课程 

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

2014年9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”

对制药工艺学教学的贡献

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1 在近二十年教学生涯中，总结教学规律，以第一作者发表教育教学论文十余篇

2 作为责任教授主持“制药工艺学”核心课程教学，该课被授予上海市精品课程

3 倡导基于最优合成路线设计，基于反应机理与反应动力学研究的药物合成工艺学习思想，贯彻并行培养专业思维与专业技能的教学理念

4 领衔或参与获得多项学校一、二等与上海市一等教学奖项

对药物与精细化学品合成工艺的贡献

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1 迭代推进非活化溴代芳烃化合物甲氧基化、烷氧基化反应发展，发明第四代绿色定量甲氧基化反应工艺，实现直接回收精甲醇 

2 以氯化锂/甲醇钠体系代替有机锂试剂作为“受阻型claisen缩合”反应缩合剂，发明多取代、全取代吡唑药效核合成方法，为药物设计与合成提供有力工具

3 系统研究对甲酚、对烷基酚的氧化反应与机理，提出完整的baik-ji式样的反应机理，为氧化手性合成奠定了基础 

4 历经十几年的认识与研究，在“前氧化”、“后氧化”路线的基础上，发明以对甲酚、溴素为原料合成香兰素的“中氧化”路线，为香兰素生产工艺的更新换代提供了可能

5 历经二十多年，在研究“单甲醚-双甲醚”、“丙烯腈苯胺缩合物”工艺的基础上，发明经典原料药甲氧苄啶第三代绿色生产工艺，推动传统药物生产工艺进步

6 基于c-h键活化，一步串联反应精准构建复杂药效核——多取代苯并噻吩并吡啶、苯并呋喃并吡啶、咔啉化合物

7 基于导向/无金属活化，以三溴化硼为硼化试剂直接进行c-h键的亲电硼化反应 

8 在研究“无溶剂法”、“异戊醇法”、“dmf-甲苯法”生产工艺基础上，开发盐酸二甲双胍第四代绿色生产工艺，推动传统药物生产工艺进步

9 提出布洛芬、磺胺嘧啶等传统药物工艺革新思想，持续推动大品种原料药绿色生产工艺进步

代表性论文
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liu x, hao lq, wang yy, yu x, yang zzy, liu yp,* ji yf.* cu₂o-catalyzed cascade phosphinylation/cyclization of 2'-aminochalcones for the synthesis of hemi-indigo derivatives. org. biomol. chem. 2024, 22, 4249–4253.   

xu xb, hao lq, liu x, wang yy, yang zzy, ding d,* ji yf.* synthesia of  via a cu-catalyzed radical cascade cyclization. synlett 2024-4-19, published online.

xu xb, wang yy, yu xiao, liu x, hao lq, ji yf.* palladium-catalyzed (3 2) annulation of aromatic acids by c(sp3)−h olefination and decarboxylative cross-coupling reaction. org. lett. 2024, 26, 13381342.  

 ji yf.*  from sulfonyl hydrazone and benzyl acrylate under transition-metal-free conditions. org. biomol. chem. 2023, 21, 7611–7615. 

hao lq, xu xb, wang yy, wu gr,* ji yf.* c−h borylation of benzophenones using hydrazone as the traceless directing group. org. lett. 2023, 25, 5875–5879. 

wang yy, liu x, xu xb, hao lq, ji yf.* palladium-catalyzed tandem diolefination reaction of benzaldehyde enabled by a remote directing group. org. lett. 2023, 25, 4962–4967.  

hao lq, wu gr, wang yy, xu xb, ji yf.* synthesis of c-3-functionalized imidazo[1,2-a]pyridines via direct para-position arylation of electron-rich anilines under transition-metal-free conditions. adv. synth. catal. 2023, 365, 2159–2164. 

hao lq, wu gr, wang yy, ji yf.* . new journal of chemistry 2023, 47, 9527–9531. 

pang bh, wang yy, hao lq, wu gr, ma zh,* ji yf.* tandem c–c/c–n bonds formation via rh(iii)-catalyzed α-fluoroalkenylation and sequential annulation of 2-arylquinazolinones and gem-difluorostyrenes. j. org. chem. 2023, 88, 143–153.

xu xb, wu gr, yang zzy, liu x, hao lq, wang yy, ma zh,* ji yf.* adamantane-1-carbonyl-directed c−h borylation and hydroxylation of benzenethiols. org. lett. 2022, 24, 7163–7167.   

wang yy, xu xb, pang bh, hao lq, wu gr, ji yf.* ligand-enabled sequential c(sp3)–h and c(sp2)–h diolefination reaction via palladium catalyst. org. lett. 2022, 24, 6734–6739. 

wu gr, yang zzy, xu xb, hao lq, chen lu, wang yy, ji yf.* metal-free boron-mediated ortho-c-h hydroxylation of n‑benzyl-3,4,5-tribromopyrazoles. org. lett. 2022, 24, 3570–3575.

wang yy, xu xb, wu gr, pang bh, liao sw,* ji yf.* ligand-enabled c−h olefination and lactonization of benzoic acids and phenylacetic acids via palladium catalyst. org. lett. 2022, 24, 821–825.

chen lu, wang zc, wang yy, hao lq, xu xb, wu gr,* ji yf.* rhodium(iii)-catalyzed cascade c−h functionalization/annulation of sulfoximines with iodonium ylides for the synthesis of cyclohexanone-1,2- benzothiazines. org. biomol. chem. 2022, 20, 887–894.

wu gr, xu xb, wang s, chen l, pang bh, ma t,* ji yf.* metal-free directed c−h borylation of 2-(n-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines. chin. chem. lett. 2022, 33, 2005–2008. 

chen l, wang zc, pang bh, wang yy, xu xb, wu gr, ji yf.* rhodium(iii)-catalyzed cascade c−h activation/annulation of ncarbamoylindoles with silyl enol ethers for the construction of dihydropyrimidoindolone skeletons. asian j. org. chem. 2021, 10, 2603–2610. 

wang yy, wu gr, xu xb, pang bh, liao sw,* ji yf.* . j. org. chem. 2021, 86, 7296–7303. 

wu gr, pang bh, wang yy, li y,chen l, ma t,* ji yf.* metal-free ortho-selective c−h borylation of 2-phenylthiopyridines using bbr_3. j. org. chem. 2021, 86, 5933–5942. 

tang sb, fu xp, wu gr, zhang ll, deng kz, yang jy, xia cc,* ji yf.* rhodium(iii)-catalyzed c4-amidation of indoleoximes with dioxazolones via c–h activation. org. biomol. chem. 2020, 18, 7922–7931.

zhang ll, deng kz, wu gr, yang jy, tang sb, fu xp, xia cc,* ji yf.* ruthenium(ii)-catalyzed α- of oxime ethers with gem-difluorostyrenes via c–h activation and c–f cleavage. j. org. chem. 2020, 85, 12670–12681. 

wu gr, fu xp, wang yy, deng kz, zhang ll, ma t,* ji yf.* by bbr₃. org. lett. 2020, 22, 7003–7007.

fu xp, wang yy, yang jy, wu gr, xia cc,* ji yf.* fully substituted pyrazoles assisted palladium-catalyzed late-stage arylation of c(sp2)-h bond. chin. j. org. chem. 2020, 40, 4305–4314.

fu xp, chen l, wu gr, liu hw, xia cc,* ji yf.* cascade access to carboline carboxylates from indolyl ketoximes and acrylates via palladium-catalyzed c–h bond alkenylation/annulation. synlett 2021, 32, 69–74. 

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, 5974–5977. 

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, 17, 7055–7065. 

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, 84, 10221–10236. 

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, 3154–3161.  

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, 702–706. 

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, 78875–78880. 

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. 2016, 42, 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. chem. 2015, 4744–4755.

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. commun. 2014,44, 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, 627–635.

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.