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发明公开
CN109053855A 一种16β-四氢吡咯基雄甾-2α-环氧-17-酮的合成方法 有权

一种16β-四氢吡咯基雄甾-2α-环氧-17-酮的合成方法
摘要：
本发明涉及医药化工技术领域，公开了一种罗库溴铵重要中间体16β‑四氢吡咯基雄甾‑2α‑环氧‑17‑酮的制备方法，所述的制备方法包括以下步骤：(1)在球磨罐中，一并加入17‑乙酰氧基雄甾‑2α,16α‑双环氧化物、吡咯烷及硅胶，在一定的机械研磨频率下进行反应；(2)反应混合物经后处理并通过重结晶得到16β‑四氢吡咯基雄甾‑2α‑环氧‑17‑酮。本发明所述的制备方法具有反应收率高、时间短、选择性好、操作简便、污染少等优点，是一种具有较好推广应用前景的绿色化学合成方法。
摘要（英）：

The invention relates to the technical field of medicines and chemical industry, discloses a preparation method of an important intermediate of rocuronium bromide, namely 16beta-tetrahydropyrrolyl androstan-2alpha-epoxy-17-one. The preparation method comprises the following steps: (1), in a ball milling tank, adding 17-acetoxy androstan-2alpha,16alpha-bisepoxide, pyrrolidine and silica gel, and reacting at a certain mechanical grinding frequency; and (2), post-treating a reaction mixture, and recrystallizing to obtain the 16beta-tetrahydropyrrolyl androstan-2alpha-epoxy-17-one. The preparationmethod has the advantages of high reaction yield, short time, high selectivity, simple and convenient operation, less pollution and the like, and is an environment-friendly chemical synthesis methodwith relatively good popularization and application prospects.

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