CN116023364A — 一种富马酸沃诺拉赞的制备方法
Assigned to Shandong Baoyuan Pharmaceutical Co ltd · Expires 2023-04-28 · 3y expired
What this patent protects
本发明公开了一种富马酸沃诺拉赞的制备方法，该制备方法以吡啶‑3‑甲醛为起始原料，首先发生溴代反应，再与吡啶‑3‑磺酰氯磺胺酰化生成5‑溴‑1‑(吡啶‑3‑基磺酸基)‑1H‑吡咯‑3‑甲醛，继续与2‑氟苯硼酸发生Suzuki偶联反应生成5‑(2‑氟苯基)‑1‑(吡啶‑3‑基磺酸基)‑1H‑吡咯‑3‑甲醛，最后经过还原胺甲基化、成盐得到富马酸沃诺拉赞。该制备方法避免使用强腐蚀性的溴素、氯化氢等物料，避免使用钯碳、雷尼镍等易燃催化剂，安全性好，且操作步骤少，适合工业化生产。
USPTO Abstract
本发明公开了一种富马酸沃诺拉赞的制备方法，该制备方法以吡啶‑3‑甲醛为起始原料，首先发生溴代反应，再与吡啶‑3‑磺酰氯磺胺酰化生成5‑溴‑1‑(吡啶‑3‑基磺酸基)‑1H‑吡咯‑3‑甲醛，继续与2‑氟苯硼酸发生Suzuki偶联反应生成5‑(2‑氟苯基)‑1‑(吡啶‑3‑基磺酸基)‑1H‑吡咯‑3‑甲醛，最后经过还原胺甲基化、成盐得到富马酸沃诺拉赞。该制备方法避免使用强腐蚀性的溴素、氯化氢等物料，避免使用钯碳、雷尼镍等易燃催化剂，安全性好，且操作步骤少，适合工业化生产。
Drugs covered by this patent
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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