A facile method for preparation of [(2)h(3)]-sufentanil and its metabolites.


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.

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@article{Srimurugan2009AFM, title={A facile method for preparation of [(2)h(3)]-sufentanil and its metabolites.}, author={Sankareswaran Srimurugan and Kaliyappan Murugan and Chinpiao Chen}, journal={Chemical & pharmaceutical bulletin}, year={2009}, volume={57 12}, pages={1421-4} }