A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist

…, OP Goel, D Johnson, S Kesten, J Knobelsdorf…

Index: Chen, Huai G.; Chung; Goel; Johnson; Kesten; Knobelsdorf; Lee; Rubin Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 5 p. 555 - 560

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Citation Number: 13

Abstract

A practical and scalable total synthesis of tachykinin NK3 receptor antagonist SR 142801,(R)-N-[1-[3-[1-benzoyl-3-(3, 4-dichlorophenyl)-3-piperidinyl] propyl]-4-phenyl-4- piperidinyl]-N-methyl acetamide 1 is described. The absolute configuration of the key intermediate 7 was determined by single crystal X-ray crystallography, on the basis of which, the absolute configuration of SR 142801 should be (R)-(+), instead of the recently ...