1-(2-HYDROXYPHENYL)-2(1H)-QUINOXALINONE DERIVATIVE SUBSTITUTED AT 7-POSITION

摘要

PURPOSE: To obtain a new compound useful as a therapeutic agent, etc., for circulatory diseases due to its possession of excellent vasodilator and hypotensive actions based on smooth muscle relaxing actions. ;CONSTITUTION: This compound of formula I (R is H, a lower alkyl, etc.; W is 0 or S; X is a halogen, cyano, etc.; Y is H, phenyl, etc.; Z is H, a hydroxy- substituted lower alkyl, etc.) or its alkali metallic salt, e.g. 7-bromo-1-(5-chloro-2- methoxyphenyl)-2-(1H)-quinoxalinone. A compound in which W is O in the compound of formula I is obtained by reacting, e.g. a compound of formula II (Z^b is H or a lower alkyl) with a compound of formula III (L¹ is amino or a lower alkoxy; L² is a halogen, a lower alkylsulfonyloxy, etc. ; R^b is H, a phenyl- substituted lower alkyl, etc.), then heating and cyclizing the resultant product at 60-150°C and subsequently oxidizing the obtained compound of formula IV with O₂ gas/alcohols at 0-50°C under acidic conditions.;COPYRIGHT: (C)1995,JPO