Synthesis of acylaminoalkenylene amides such as (4R)-4-[N'-methyl-N'-(3,5-bistrifluoromethyl-benzoyl)-amino]-4(-3,4-dichlorobenzyl)-but-2-enoic acid N-[(R)-epsilon-caprolactam-3-yl]-amide hemihydrate useful as substance P antagonists

摘要

Disclosed is a process for preparing compounds of formula I, or a solvate or hydrate thereof, where R is phenyl; R1 is hydrogen or C1-C7-alkyl; R2 is hydrogen, C1-C7-alkyl or phenyl; R3 is phenyl, naphthyl, 1H-indol-3-yl or 1-C1-C7-alkyl-indol-3-yl; and R5 is C3-C8-cycloalkyl, D-azacycloheptan-2-on-3-yl or L-azacycloheptan-2-on-3-yl, and the substituents can be substituted as defined in the specification. The compounds produced by the process are useful in the treatment of conditions associated with substance P and neurokinin.