CAS: 1187594-09-7; 2-(3-(4-(3H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1H-Pyrazol-1-yl)-1-(Ethylsulfonyl)Azetidin-3-yl)Acetonitrile

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CAS号1187595-84-1 巴瑞克替尼磷酸盐

巴瑞克替尼中间体3置于1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 乙醇 用作溶剂,化学反应 3.0H,以9.3 G的收率获得巴瑞替尼
参考文献:一种巴瑞替尼的制备方法
标题:一种巴瑞替尼的制备方法
摘要:本发明公开了一种巴瑞替尼的制备方法;以(4‑氯‑7H‑吡咯并[2,3‑d]嘧啶‑7‑基)新戊酸甲酯为起始物料,与1‑(1‑乙氧基乙基)‑4‑(4,4,5,5‑四甲基‑1,3,2‑二氧杂硼烷‑2‑基)‑1H‑吡唑经偶联,酸解,加成反应得到(4‑(1‑(3‑(氰基甲基)‑1‑(乙基磺酰基)氮杂环丁烷‑3‑基)‑1H‑吡唑‑4‑基)‑7H‑吡咯并[2,3‑d]嘧啶‑7‑基)新戊酸甲酯;再经碱解反应,精制得到巴瑞替尼.碱解反应采用了dbu等有机碱进行水解脱保护反应,得到的巴瑞替尼纯度高,收率好,其中羟甲基中间体杂质g降低至0.15%以下,经精制工序后,得到的巴瑞替尼原料药纯度可达99.9%,易于工业化生产.

专利信息

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

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).