CAS: 2326521-71-3; 2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-Methylpyrrolidin-2-yl)Methoxy)-5,6,7,8-Tetrahydropyrido[3,4-D]Pyrimidin-4-yl)-1-(2-Fluoroacryloyl)Piperazin-2-yl)Acetonitrile

7-苄基-5,6,7,8-四氢吡啶并[3,4-D]嘧啶-2,4(1H,3H)-二酮置于盐酸,Tris-(Dibenzylideneacetone)Dipalladium(0),10 Wt% Pd(Oh)2 On Carbon,氢气,Sodium Methylate,Palladium Diacetate,Sodium Hydride,Caesium Carbonate,R-(+)-1,1'-联萘-2,2'-双二苯膦,三乙胺,N,N-二异丙基乙胺,乙硫醇,三氯氧磷,2-二环己基磷-2',6'-二异丙氧基-1,1'-联苯体系中,用 甲醇,二氯甲烷,N,N-二甲基乙酰胺,水,N,N-二甲基甲酰胺,甲苯 用作溶剂,-40.0~110.0 °C,310.27 Kpa 条件下,反应 81.25H,反应生成(2S)-4-[7-(8-氯-1-萘)-5,6,7,8-四氢-2-[[((2S)-1-甲基-2-吡咯烷基]甲氧基]吡啶基[3,4-D]嘧啶-4-基]-1-(2-氟-1-氧代-2-丙烯-1-基)-2-哌chemicalbook嗪乙腈;2-((S)-4-(7-(8-氯萘-1-基)-2-((((S)-1-
参考文献: Crystalline Forms Of A Kras G12C Inhibitor[fr] Formes Cristallines D'Un Inhibiteur De Kras G12C
标题: Crystalline Forms Of A Kras G12C Inhibitor[fr] Formes Cristallines D'Un Inhibiteur De Kras G12C
摘要:本发明涉及kras G12C抑制剂及其盐的晶型.具体而言,本发明涉及kras Gt2C抑制剂2-[(2S)-4-[7-(8-氯-1-萘基)-2-[[(2S)-1-甲基吡咯烷-2-基]甲氧基]-6,8-二氢-5H-吡啶[3,4-D]嘧啶-4-基]-1-(2-氟丙-2-烯酰基)哌嗪-2-基]乙腈的晶型,以及包含该晶型的制药组合物,制备该晶型的方法和使用方法.

专利信息

专利号:US-2025101006-A1
优先权日:2022-01-31
标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents
发明人：BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO
权利人:NOVARTIS AG
摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.

专利号:US-2025115551-A1
优先权日:2023-10-03
标 题:Synthesis of ras inhibitors
发明人：LI YI; MENDOZA BENJAMIN; NAGANATHAN SRIRAM; WANG ROSS; YI YI; BALLMER STEVEN G; DAVIDSON JAMES; HUANG XIAOJUN
权利人:REVOLUTION MEDICINES INC
摘要:The present invention relates to Ras inhibitors, intermediates in the synthesis thereto, and methods for preparing the Ras inhibitors and the intermediates.

专利号:US-2024400558-A1
优先权日:2021-09-09
标题 :Processes and intermediates for synthesis of adagrasib
发明人：SCATTOLIN THOMAS; CHEN CHENG; GHARBAOUI TAWFIK; GAN YONGHONG; ACHMATOWICZ MICHAL; SNEAD DAVID
权利人:MIRATI THERAPEUTICS INC
摘要:The present invention relates to improved synthetic routes of synthesizing adagrasib. The invention also provides intermediates used in the provided synthetic routes.

专利号:WO-2023205074-A1
优先权日:2022-04-18
标 题:Processes and intermediates for synthesis of adagrasib
发明人：SCATTOLIN THOMAS; GAN YONGHONG; CHEN CHENG; CHEN CHENGSHENG
权利人:MIRATI THERAPEUTICS INC
摘要:The present invention relates to new synthetic routes of synthesizing adagrasib. The invention also provides intermediates used in the provided synthetic routes.

专利号:WO-2024163626-A3
优先权日:2023-01-31
标题:Processes and intermediates for synthesis of adagrasib
发明人：SCATTOLIN THOMAS; CHEN CHENG; GAN YONGHONG; CHEN CHENGSHENG; LU ZHICHAO
权利人:MIRATI THERAPEUTICS INC
摘要:The present invention relates to new synthetic routes of synthesizing adagrasib. The invention also provides intermediates used in the provided synthetic routes.

专利号:WO-2023143605-A1
优先权日:2022-01-31
标 题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents