PURPOSE: To obtain a new catechol derivative having excellent antiinflammatory action, immunoregulatory action, analgesic action, antipyretic action, bronchodilating action, etc.
CONSTITUTION: This catechol derivative is expressed by formula I [one of R1 and R2 is a lower alkyl and the other is H, a lower alkyl, a cycloalkyl, etc.; R3 is H, a lower alkyl, phenyl or NR4R5 (R4 and R5 each is H, a lower alkyl, etc.); A is O or S; Z is N and Y is C-R6 (R6 is H or a lower alkyl) when A is O and Y is N and Z is C-R7 (R7 is H or a lower alkyl) when A is S; B is single bond or a lower alkylene; excluding the case that A is S, B is single bond and both of R1 and R2 are lower alkyl], e.g. 5-amino-3-(3-cyclopentyloxy-4- methoxybenzyl)isoxazole. The compound of formula I can be produced by reacting a compound of formula II [one of R1a and R2a is a lower alkyl and the other is a (phenyl)lower alkyl, etc.; E is a lower alkyl) with a nitrile derivative of formula R6-CH2-CN and cyclizing the produced compound of formula III with hydroxylamine.
TANAKA AKIE
GOTO KIYOTO
