CAS: 1792180-81-4; 1-((2S,5R)-5-((7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Amino)-2-Methylpiperidin-1-yl)Prop-2-En-1-One

2,4-二氯-7H吡咯[2,3-D]嘧啶置于potassium Phosphate,10% Palladium Hydroxide On Charcoal,氢气,Potassium Carbonate体系中,用 四氢呋喃,水 用作溶剂,5.0~90.0 °C,380.01 Kpa 条件下,反应 34.0H,反应生成1-[(2S,5R)-2-甲基-5-(7H-吡咯并[2,3-D]嘧啶-4-基氨基)-1-哌啶基]-2-丙烯-1-酮丙二酸酯
参考文献:选择性jak3共价抑制剂pf-06651600的工艺开发和规模放大
标题:选择性jak3共价抑制剂pf-06651600的工艺开发和规模放大
摘要:通过成功启用第一代合成技术,已经开发了pf-06651600(1)的可扩展过程.合成亮点包括:(1)用较便宜的5%rh / C催化剂代替昂贵的pto 2进行吡啶加氢;(2)鉴定非对映体盐结晶,以便直接从对映体中分离出对映体纯的顺式异构体.顺式/反式异构体的外消旋混合物,(3)通过schotten-Baumann条件产生高产率的酰胺化反应,以及(4)稳定结晶盐(1.tsoh)的可重现结晶过程的关键发展),适合长期存放和片剂配制.消除了所有色谱纯化,包括两次手性sfc色谱分离.与合成的每个步骤中的其他改进相结合,总产率从5%提高到14%.已交付了几百千克的api多批次产品,以支持临床研究.
Doi:10.1021/acs.Oprd.9B00198

专利信息

专利号:JP-2835630-B2
优先权日:1988-06-20
标 题 :Nucleoside derivatives that can be used in the synthesis of targeted oligonucleotides, oligonucleotides derived from these derivatives, and their synthesis

专利号:JP-H03505209-A
优先权日:1988-06-20
标题:Nucleoside derivatives that can be used in the synthesis of targeted oligonucleotides, oligonucleotides obtained from these derivatives, and their synthesis

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

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).

专利号:CN-119060058-A
优先权日:2024-08-21
标 题:Synthesis method of Li Texi tenib tosylate