CN109180589A — 玻玛西尼中间体的制备方法
Assigned to Wuhan Institute of Technology · Expires 2019-01-11 · 7y expired
What this patent protects
本发明涉及抗乳腺癌药物玻玛西尼(Bemaciclib)的重要中间体：6‑溴‑4‑氟‑1‑异丙基‑2‑甲基‑1H‑苯并[d]咪唑的制备方法，以4‑溴‑2,6‑二氟苯胺和N‑异丙基乙酰胺为起始反应原料，经过西佛碱加成反应，转化为(4‑溴‑2,6‑二氟苯基)‑N‑异丙基乙酰亚胺，再经过催化关环，生成1H‑苯并(d)咪唑环中间体6‑溴‑4氟‑1‑异丙基‑2‑甲基‑1H‑苯并[d]咪唑。本发明的有益效果：本发明以廉价易得、环保的碱金属碳酸盐为催化剂，节约了工艺成本，有利于环境保护，小试、中试一步产率达到80％以上，更适合于工业化生产。
USPTO Abstract
本发明涉及抗乳腺癌药物玻玛西尼(Bemaciclib)的重要中间体：6‑溴‑4‑氟‑1‑异丙基‑2‑甲基‑1H‑苯并[d]咪唑的制备方法，以4‑溴‑2,6‑二氟苯胺和N‑异丙基乙酰胺为起始反应原料，经过西佛碱加成反应，转化为(4‑溴‑2,6‑二氟苯基)‑N‑异丙基乙酰亚胺，再经过催化关环，生成1H‑苯并(d)咪唑环中间体6‑溴‑4氟‑1‑异丙基‑2‑甲基‑1H‑苯并[d]咪唑。本发明的有益效果：本发明以廉价易得、环保的碱金属碳酸盐为催化剂，节约了工艺成本，有利于环境保护，小试、中试一步产率达到80％以上，更适合于工业化生产。
Drugs covered by this patent
- Verzenio (abemaciclib) · Eli Lilly
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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