一种枸橼酸托法替布中间体的制备方法
本发明提供了一种枸橼酸托法替布中间体的制备方法,属于医药化工技术领域。本发明以3‑卤代‑4‑甲基吡啶为原料,经亲核取代、苄卤保护、硼氢化物还原、手性拆分、游离、成盐制得(3R,4R)‑1‑苄基‑3‑甲氨基‑4‑甲基‑哌啶双盐酸盐。本发明利用硼氢化合物作为还原剂,将1‑苄基‑3‑甲氨基‑4‑甲基吡啶盐酸盐的吡啶环还原为哌啶环,降低了生产成本。本发明的合成方法反应条件温和、操作简单,适合大规模工业化生产。
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