182621-57-4Relevant articles and documents
A reliable and efficient synthesis of SR 142801
Giardina,Grugni, Mario,Rigolio, Roberto,Vassallo, Marco,Erhard, Karl,Farina, Carlo
, p. 2307 - 2310 (2007/10/03)
A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801, (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1 -yl}-4-phenylpiperidin-4-yl}-N-methylacetamide [(S)-(+)-(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5 via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen.