Bioorganic and Medicinal Chemistry Letters p. 2307 - 2310 (1996)
Update date:2022-08-02
Topics:
Giardina
Grugni, Mario
Rigolio, Roberto
Vassallo, Marco
Erhard, Karl
Farina, Carlo
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.
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