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Telescoped Procedure for Buprenorphine Manufacturing Process

有机合成与工艺文献分享 2025-08-27 06:58

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背景：丁丙诺啡制备过程涉及六步化学反应，起始原料为蒂巴因，其中第一阶段产物常含C-7异构体杂质。研究目的：开发连续流工艺以规避剧毒试剂甲基乙烯基酮的使用，并解决中间体在异丙醇中溶解度低的问题。结论：通过添加THF共溶剂实现选择性蒸馏，结合钯碳氢化与结晶工艺优化，成功建立体积效率更高的连续化生产路径，最终产物经80℃晶种诱导后可在10℃高效析出。

Telescoped Procedure for Buprenorphine Manufacturing Process

查看文献： Development of a Telescoped Procedure for Stages 1 and 2 of the Buprenorphine Manufacturing Process
查看期刊： Organic Process Research & Development

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