CAS: 113237-20-0; 2,6-Dichloro-5-Fluoronicotinamide

相似化合物

82671-02-1 62068-78-4 771581-97-6

上下游产品

2,6-dichloro-5-fluoro-pyridine-3-carbonitrile 5-fluoro-2,6-dihydroxynicotinamide 2-Cyanopyridine 1,2-dichloro-ethane 2,6-dichloro-5-fluoro-3-pyridinecarboxylic acid 2,6-dichloro-5-fluoropyridine-3-amine tert-butyl 4,6-dichloro-7-fluoro-3-oxo-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxylate 4,6-dichloro-7-fluoro-1H-pyrrolo[3,4-c]pyridin-3(2H)-one

2,6-二氯-5-氟烟酸置于草酰氯,Ammonium Hydroxide体系中,用 二氯甲烷,N,N-二甲基甲酰胺,1,4-二氧六环 用作溶剂,化学反应 16.5H,以50%的收率获得2,6-二氯-3-甲酰胺-5-氟吡啶
参考文献:发现用于治疗实体瘤的krasg12C(amg 510)共价抑制剂.
标题:发现用于治疗实体瘤的krasg12C(amg 510)共价抑制剂.
摘要:Krasg12C已成为治疗实体瘤的有希望的靶标.靶向突变半胱氨酸12残基的共价抑制剂已显示出可以通过这个长期的"不可吸收的"靶标破坏信号传导.然而,尚未确定临床上可行的抑制剂.在这里,我们报告了开发利用我们在krasg12C中鉴定出的隐窝(h95 / Y96 / Q99)的努力,以鉴定适合临床开发的抑制剂.描述了基于结构的设计努力,该努力导致鉴定了新颖的喹唑啉酮支架,以及克服了围绕轴向手性联芳基键旋转受限而引起的构型稳定性问题的优化努力.对产生的潜在生物进行生物制药优化,最终鉴定出了amg 510,这是一种高效,选择性强,
Doi:10.1021/acs.Jmedchem.9B01180

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-2023192682-A1
优先权日:2019-11-14
标题:Improved synthesis of kras g12c inhibitor compound

专利号:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:WO-2020102730-A1
优先权日:2018-11-16
标 题:Improved synthesis of key intermediate of kras g12c inhibitor compound

专利号:US-11299491-B2
优先权日:2018-11-16
标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound