Method is used to prepare -7-/(1S) -1 hydroxyl -1,2 of 7,8 dihydros of (6R, 7R, 14S) -17-CYCLOPROPYLMETHYL, 2 TRIMETHYLPROPYL/-6-0- methyl -6,14- ethano- -17- normorphines

摘要

Method prepares (6R, 7R, 14S) -17-cyclopropylmethyl 7,8-dihydro-7-/(1s) -1-hydroxy-1,2,2-trimethylpropyl/ -6-0-methyl-6, the 14-ethano-17-normorphine of general formula I, as strong anodyne (buprenorphine). Synthesize including while cracking the acylation secondary amide generation of main functional group and hydrolysis cyane group bies alkaline hydrated oxide passes through complex hydride by cyclopropyl carbonyl chloride and subsequent reduction generation amide; possible direct alkylation secondary amide is by Cvclopropvlmethvl halide, and double bond. of final catalysis reduction inner ringIMAGE