CN104610254B — 一种帕博赛布的低成本制备方法
Assigned to Xinfa Pharmaceutical Co Ltd · Expires 2017-02-01 · 9y expired
What this patent protects
本发明涉及一种帕博赛布的低成本制备方法。该方法是以2,4‑二氯‑5‑氰基嘧啶为起始原料，通过氰基格氏化、水解得5‑乙酰基‑2,4‑二氯嘧啶，保护羰基后再胺化，脱羰基，然后用双乙烯酮与胺基进行酰化反应得5‑乙酰基‑4‑乙酰乙酰胺基‑2‑氯嘧啶；该产物通过分子内脱水得6‑乙酰基‑8‑环戊基‑5‑甲基‑2‑氯‑8H‑吡啶并[2,3‑d]嘧啶‑7‑酮，羰基保护6位乙酰基后再与胺基吡啶衍生物反应，得4‑{6‑[6‑1,1二烷氧基)乙基‑8‑环戊基‑5‑甲基‑7‑酮‑7,8二氢吡啶并[2,3‑d]嘧啶‑2‑胺基]‑吡啶‑3‑基}‑哌嗪‑1‑羧酸叔丁酯，最后酸水解、中…
USPTO Abstract
本发明涉及一种帕博赛布的低成本制备方法。该方法是以2,4‑二氯‑5‑氰基嘧啶为起始原料，通过氰基格氏化、水解得5‑乙酰基‑2,4‑二氯嘧啶，保护羰基后再胺化，脱羰基，然后用双乙烯酮与胺基进行酰化反应得5‑乙酰基‑4‑乙酰乙酰胺基‑2‑氯嘧啶；该产物通过分子内脱水得6‑乙酰基‑8‑环戊基‑5‑甲基‑2‑氯‑8H‑吡啶并[2,3‑d]嘧啶‑7‑酮，羰基保护6位乙酰基后再与胺基吡啶衍生物反应，得4‑{6‑[6‑1,1二烷氧基)乙基‑8‑环戊基‑5‑甲基‑7‑酮‑7,8二氢吡啶并[2,3‑d]嘧啶‑2‑胺基]‑吡啶‑3‑基}‑哌嗪‑1‑羧酸叔丁酯，最后酸水解、中和得帕博塞布游离碱。本发明使用原料易得，成本低，安全环保。
Drugs covered by this patent
- Palbociclib (palbociclib) · Pfizer Inc.
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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