To obtain the subject new compound having an antagonism against a substance P and neurokinin A.
This compound is expressed by formula I or formula II [R1 and R2 are each a (substituted) aryl or heteroryl; A is methylene, carbonyl or sulfonyl; B is a single bond, a 1-4C alkylene or the like, D is O or S; E is a 1-6C alkylene or the like; G is a 1-4C alkylene; L is a group having the formula: -N(R3)-(R3 is an aryl or the like); R7 is a lower alkyl], e.g. 1-{2-[2-(3,4- dichlorophenyl)-4-(3-methoxybenzoyl)morpholin-2-yl]ethyl}-4-phenylpiperidine-4- carboxylic acid amide. The compound of formula I or formula II is obtained by subjecting an alcohol derivative of formula III to Swern oxidation preferably in methylene chloride at -100°C to a room temperature for 10 min-2 days to obtain an aldehyde derivative of formula IV and subjecting the resultant compound and a compound of formula V to a reducing amination reaction, preferably using hydrogenated sodium cyanoborate at -10°C to +100°C.
FUKAZAWA TETSUYA
KURATA HITOSHI
ISHIBASHI KIMIKI
NAKAJIMA KATSUYOSHI
YAMAGUCHI TAKESHI
ITO KAZUHIRO
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