| 摘要 |
New preparation of glutaramides of formula (I), their salts and enantiomers, comprises cyclisation of compounds of formula (III). Ar = phenyl (optionally substituted by one or more halo, OH, 1-4C alkoxy, CF3 or 1-4C alkyl); pyridyl; or thienyl; X = methylene or ethylene; and Y = CN or carboxy. (I) is isolated as the salt or the acid. Glutaramides of formula (I) are new, provided that when X is methylene then Ar is not unsubstituted phenyl, and that when X is ethylene then Ar is not unsubstituted phenyl or phenyl substituted in position 2 by methyl or in position 4 by Cl, Br, F, methyl, or methoxy. Also claimed are the optically active salts and enantiomers of (I) (without provisos). Starting materials of formula (III) are new, provided that when X = ethylene and Y = carboxy then Ar is not unsubstituted phenyl or phenyl substituted in position 3 by methoxy or 3,4-disubstituted by methoxy. Also claimed are the optically active salts and enantiomers of (III) (without provisos). #CMT#USE : #/CMT# (I) is used to prepare a 3,3-disubstituted piperidine of formula (A), especially (-)-3-(3,4-dichlorophenyl)-3-(2-hydroxyethyl)-piperidine; or (+)-3-(3,4-dichlorophenyl)-3-(3-hydroxypropyl)-piperidine. (A) are starting materials for the preparation of neurokinin antagonists. #CMT#ADVANTAGE : #/CMT# (I) are easily resolved and then transformed to optically pure (A). |
