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.
Srimurugan
Sankareswaran
S
Department of Chemistry, National Dong Hwa University, Hualien, Taiwan.
Murugan
Kaliyappan
K
Chen
Chinpiao
C
D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry; D017409:Sufentanil / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry
D000700:Analgesics; D010165:Palladium; C047304:desmethylsufentanil; D017409:Sufentanil