A facile method for preparation of [2H3]-sufentanil and its metabolites

S Srimurugan, K Murugan, C Chen

文献索引：Srimurugan, Sankareswaran; Murugan, Kaliyappan; Chen, Chinpiao Chemical and Pharmaceutical Bulletin, 2009 , vol. 57, # 12 p. 1421 - 1424

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被引用次数: 9

摘要

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 optimized process.