CAS: 248281-84-7; 5-Chloro-N-Ethyl-4-Hydroxy-1-Methyl-2-Oxo-N-Phenyl-1,2-Dihydroquinoline-3-Carboxamide

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CAS号103-69-5 N-乙基苯胺 | CAS号335640-50-1 5-CHLORO-1,2-DI... | CAS号637027-41-9 5-氯-4-羟基-1-甲基-2... | CAS号20829-96-3 5-氯-1H-苯并[d][1,... | CAS号2148-56-3 2-氨基-6-氯苯甲酸 | CAS号40707-01-5 5-氯-1-甲基-1H-苯并[... | CAS号248282-10-2 5-氯-1,2-二氢-4-羟基... | CAS号142613-14-7 methyl 3-(N-eth... | CAS号118081-77-9 3-(Ethyl(phenyl... | CAS号637027-41-9 5-氯-4-羟基-1-甲基-2...

5-氯-1,2-二氢-4-羟基-1-甲基-2-氧代-3-喹啉羧酸乙酯 以 正庚烷 用作溶剂,化学反应 6.68H,反应生成拉喹莫德
参考文献:拉喹莫德,喹啉-3-羧酰胺的合成和反应性:烯醇质子到氮原子的分子内转移作为可能的乙烯形成机理.
标题:拉喹莫德,喹啉-3-羧酰胺的合成和反应性:烯醇质子到氮原子的分子内转移作为可能的乙烯形成机理.
摘要:5-氯-N-乙基-1,2-二氢-4-羟基-1-甲基-2-氧代-N-苯基-3-喹啉甲酰胺(laquinimod,2)是临床试验中的口服药物,可用于治疗多种硬化.合成2的最后一步是酯1与n-乙基苯胺的高产氨解反应.在1和2之间存在平衡,并且在反应过程中除去生成的甲醇是从1获得2的高收率的先决条件.1和2的反应性用力学模型解释了该机理,该模型涉及烯醇质子转移到环外羰基取代基并伴随形成烯酮3.由于2,由于空间相互作用,使与羰基氧的分子内氢键减弱,因此特别有利于2的质子转移.既1和2经历solvolosis反应服从一级反应动力学,进一步支持该理论认为这两种分子都能够单分子分解成烯酮3.的依赖于溶剂的分光设有2表明该分子主要存在于两个构象中.一种构象在非极性溶剂中是有利的,并且可能是分子内氢键合的结果.在极性溶剂中有利于另一种构象,并且可能表现出较少的分子内氢键.
Doi:10.1021/jo052368Q

专利信息

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-10906888-B2
优先权日:2016-07-14
标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
发明人：CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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).

专利号:US-2025250277-A1
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 M; 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; CAMP HEIDI S; PADLEY ROBERT J; VOSS JEFFREY W; PANGAN AILEEN L
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 vasculitis), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating giant cell arteritis (GCA).