CAS: 1310726-60-3; (3S,4R)-3-Ethyl-4-(3H-Imidazo[1,2-A]Pyrrolo[2,3-E]Pyrazin-8-yl)-N-(2,2,2-Trifluoroethyl)Pyrrolidine-1-Carboxamide

上下游产品

trifluoroethylamine 1,1'-carbonyldiimidazole (3R,4S)-benzyl 3-(2-bromoacetyl)-4-ethylpyrrolidine-1-carboxylate 2-bromo-5-(p-toluenesulfonyl)-5H-pyrrolo[2,3-b]pyrazine

(3S,4R)-3-Ethyl-4-(3-Tosyl-3H-Imidazo[1,2-A]Pyrrolo[2,3-E]Pyrazin-8-yl)-N-(2,2,2-Trifluoroethyl)Pyrrolidine-1-Carboxamide置于水,Sodium Hydroxide体系中,用 1,4-二氧六环 用作溶剂,化学反应 1.0H,以5.52 G的收率获得乌帕替尼
参考文献: Alternate Processes For The Preparation Of Pyrrolidine Derivatives[fr] Procédés Alternatifs Pour La Préparation De Dérivés De Pyrrolidine
标题: Alternate Processes For The Preparation Of Pyrrolidine Derivatives[fr] Procédés Alternatifs Pour La Préparation De Dérivés De Pyrrolidine
摘要:本申请涉及一种用于制备吡咯烷衍生物的过程,该衍生物可用作活性成分的关键中间体.具体方面涉及一种用于制备upadacitinib中间体4-乙基吡咯烷-3-羧酸,其酯或其盐的替代过程.与已知过程相比,本文披露的过程具有成本效益且在工业上可行.

专利信息

专利号:US-11926633-B2
优先权日:2018-08-31
标 题:Synthesis methods for upadacitinib and intermediate thereof
发明人：WANG PENG; LI PIXU; WEI QIANG; CHENG WEN; WU HAO
权利人:SUZHOU PENGXU PHARMATECH CO LTD
摘要:The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III),wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.

专利号:WO-2025149011-A1
优先权日:2024-01-11
标 题:Synthesis process for upadacitinib or hydrate thereof
发明人：WANG PINGZHONG; YANG ZHENGYI; WANG YAO; GU HONG; SU HU; HUANG LUNING
权利人:ZHEJIANG HUAHAI PHARM CO LTD
摘要:Provided is a synthesis process for Upadacitinib or a hydrate thereof, relating to the field of drug synthesis. The synthesis process specifically comprises: reacting a compound of formula (2) and a compound of formula (3) in an organic solvent and water, and upon completion of the reaction, mixing a reaction system with inorganic alkali A for reaction to obtain a compound of formula (1) or a hydrate thereof. The method involves simple and convenient operations, the product is easy to obtain, the product has high purity, and amplified production and large-scale production can be stably realized.

专利号:US-11993606-B2
优先权日:2015-10-16
标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
发明人：MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÃœNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).

专利号:US-11976077-B2
优先权日:2015-10-16
标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof
发明人：PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÃœNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.

专利号:US-11512092-B2
优先权日:2015-10-16
标题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
发明人：ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÃœNDER BEN
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).

专利号:US-11524964-B2
优先权日:2015-10-16
标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
发明人：MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÃœNDER BEN; PANGAN AILEEN L; SONG IN-HO
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).