Process for the preparation of 4-fluoro-alpha-[2-methyl-1-oxopropyl]-N-oxo-N, beta-diphenylbenzamides
By employing specific catalysts and solvents through the Heck reaction and selective α-addition reaction, the synthetic route of atorvastatin calcium nucleus was simplified, solving the problems of incomplete conversion of raw materials and high impurity content. This resulted in the synthesis of atorvastatin nucleus with high yield and high purity, making it suitable for industrial production.
CN122404174APending Publication Date: 2026-07-17JIANGSU ALPHA PHARM CO LTD
Patent Information
- Application Number
- CN202610575089.7
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-04-28
- Publication Date
- 2026-07-17
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Figure CN122404174A_ABST
Abstract
本发明公开了一种4‑氟‑α‑[2‑甲基‑1‑氧丙基]‑ν‑氧代‑N,β‑二苯基苯丁酰胺制备工艺，第一步反应，化合物Ⅰ与化合物Ⅱ在80～100℃下催化加热反应12～24h，得到化合物Ⅲ；第二步反应，化合物Ⅲ与化合物Ⅳ，在催化剂及还原剂作用下，室温下搅拌反应12～16h，得到化合物Ⅴ。本发明的有益效果是：本发明的反应通过heck反应构建双键链接，再通过选择性的α位加成反应，得到阿托伐他汀母核，路线新颖，反应原料易得，属于新的反应路线，为阿托伐他汀母核的合成提供了新的研究方向；本发明的反应路线简单，反应步骤少，反应选择性高，产物收率高，副产物少，原子经济性好，后处理方便，简化了工艺操作，降低了成本，适合工业化扩大规模生产。
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Citation Information
Patent Citations
Process for preparation of 4-fluoro-α-[2methyl-l-oxopropyl]-γ-oxo—N—β-diphenylbenzene butane amide
US8946479B2