作者:Sankareswaran Srimurugan、Kaliyappan Murugan、Chinpiao Chen
DOI:10.1248/cpb.57.1421
日期:——
An improved process for the synthesis of sufentanil with an overall yield of 26% is described. The reactive and high yielding N-debenzylation of the piperidine intermediate 7 using a mixture of Pd/C and Pd(OH)(2) was applied to other drug intermediates affording free amines in short reaction times. The deuterium-labeled sufentanil and the metabolite desmethylsufentanil were synthesized applying the
描述了一种合成舒芬太尼的改进方法,总产率为26%。使用Pd / C和Pd(OH)(2)的混合物将哌啶中间体7进行反应性高收率的N-脱苄基化反应,并将其应用到可在短反应时间内提供游离胺的其他药物中间体上。通过优化工艺合成了氘标记的舒芬太尼和代谢产物去甲基舒芬太尼。