CN105037236B — 瑞博西尼中间体及其制备方法
Assigned to Beijing Huazhong Enkang Medicine Technology Co.,Ltd. · Expires 2017-07-28 · 9y expired
What this patent protects
本发明揭示了一种制备瑞博西尼(Ribociclib)的中间体N‑环戊基‑2‑甲氧基‑5‑(N,N‑二甲基‑甲酰胺基)‑3‑吡咯甲腈(II)及其制备方法，其制备步骤包括：N,N‑二甲基‑2‑羰基‑丙酰胺(IV)经卤代反应得到N,N‑二甲基‑1‑卤素‑2‑羰基‑丙酰胺(V)；中间体V与丙二腈发生取代反应制得N,N‑二甲基‑1,1‑二腈基‑3‑羰基‑丁酰胺(VI)；中间体VI经环合反应制得2‑甲氧基‑5‑(N,N‑二甲基‑甲酰胺基)‑3‑吡咯甲腈(VII)；中间体VII与溴代环戊烷发生偶联反应得到制备瑞博西尼中间体N‑环戊基‑2‑甲氧基‑5‑(N,N‑二甲基‑…
USPTO Abstract
本发明揭示了一种制备瑞博西尼(Ribociclib)的中间体N‑环戊基‑2‑甲氧基‑5‑(N,N‑二甲基‑甲酰胺基)‑3‑吡咯甲腈(II)及其制备方法，其制备步骤包括：N,N‑二甲基‑2‑羰基‑丙酰胺(IV)经卤代反应得到N,N‑二甲基‑1‑卤素‑2‑羰基‑丙酰胺(V)；中间体V与丙二腈发生取代反应制得N,N‑二甲基‑1,1‑二腈基‑3‑羰基‑丁酰胺(VI)；中间体VI经环合反应制得2‑甲氧基‑5‑(N,N‑二甲基‑甲酰胺基)‑3‑吡咯甲腈(VII)；中间体VII与溴代环戊烷发生偶联反应得到制备瑞博西尼中间体N‑环戊基‑2‑甲氧基‑5‑(N,N‑二甲基‑甲酰胺基)‑3‑吡咯甲腈(II)。该中间体II与N‑[5‑(1‑哌嗪基)‑2‑哌啶基]胍(III)发生缩合反应制得瑞博西尼。该制备方法原料易得，工艺简洁，经济环保，适合工业化生产。
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Bibliographic data sourced from FDA Orange Book + USPTO public records. Plain-English summary generated by AI grounded in source text. Patent term extensions (PTR, SPC, pediatric) may shift the effective expiry. Not legal advice.
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