CAS: 1016636-76-2; 6-Bromo-2-Chloro-8-Cyclopentyl-5-Methylpyrido[2,3-D]Pyrimidin-7(8H)-One

上下游产品

2-chloro-5-methyl-8-cyclopentylpyridin[2,3-d]pyrimidin-8-hydro-7-one Cyclopentamine 5-bromo-2-chloro-N-cyclopentylaminopyrimidine-4-amine triethyl bromophosphonoacetate tertbutyl 4(6((6bromo8cyclopentyl5methyl7oxo7,8dihydropyrido[2,3d]pyrimidin2yl)amino)pyridin3yl)piperazine1carboxylate tertbutyl 4(6((6(1butoxyvinyl)8cyclopentyl5methyl7oxo7,8dihydropyrido[2,3d]pyrimidin2yl)amino)pyridin3yl)piperazine1carboxylate PD 0332991 4-[6-(6-acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)pyridine-3-yl]piperazine-1-carboxylic acid tert-butyl ester

5-溴-2-氯-N-环戊基-4-嘧啶胺置于n-溴代丁二酰亚胺(Nbs),Palladium Diacetate,草酸,乙酸酐,三乙胺体系中,用 N-甲基吡咯烷酮,乙腈 用作溶剂,化学反应生成6-溴-2-氯-8-环戊基-5-甲基-吡啶并[2,3-D]嘧啶-7(8H)-酮
参考文献:Palbociclib商业制造工艺开发.第一部分:格氏试剂的s N Ar偶联中区域选择性的控制
标题:Palbociclib商业制造工艺开发.第一部分:格氏试剂的s N Ar偶联中区域选择性的控制
摘要:这是描述palbociclib(1)的商业制造工艺开发的三篇系列文章中的第一篇.该手稿侧重于氨基吡啶3和氯嘧啶7之间的s N Ar偶联.从合成和机理的角度研究了s N Ar偶联的区域选择性.Grignard碱被确定为该反应的优选碱类,从而简化了工艺并降低了氨基吡啶3的使用率.本s的发展ñ氩反应为可缩放的商业制造过程也被描述.
Doi:10.1021/acs.Oprd.6B00070

专利信息

专利号:US-10807978-B2
优先权日:2016-07-04
标题:Process for preparation of palbociclib
发明人：MURUGAN ANDIAPPAN; KABRA VIPINKUMAR SHRIRAM; GADE CHINNA SAIDA REDDY; GONDU RAMA RAO; CHANDRASHEKAR SHRAVANKUMAR; PASUPATHY KRISHNAMOORTHY; KALAISELVAN ANANDAN
权利人:Dr Reddys Laboratories Ltd
摘要:The present application relates to a process for the preparation of crystalline form A of palbociclib having specific surface area more than 2 m 2 /g comprising one-pot process for the preparation of compound of formula (IV). The present application further relates to the preparation of acid-addition salts of palbociclib and their use for the synthesis of crystalline form A of palbociclib having specific surface area more than 2 m 2 /g.

专利号:US-7781583-B2
优先权日:2006-09-08
标题:Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d] pryimidin-7-ones
发明人：ERDMAN DAVID THOMAS; FLAMME CATHLIN MARIE; NELSON JADE DOUGLAS
权利人:PFIZER
摘要:The present invention provides methods of preparing substituted 2-(pyridin-2-ylamino)-pirido[2,3-d]pyrimidin-7-ones (formula 1), n nuseful in treating cell proliferative disorders, or a pharmaceutically acceptable salt thereof.

专利号:US-2008125588-A1
优先权日:2006-09-08
标 题:SYNTHESIS OF 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3-d] PRYIMIDIN-7-ONES

专利号:CN-112961152-B
优先权日:2020-02-26
标 题 :Synthesis method of palbociclib impurity