PURPOSE: To obtain advantageously the titled compound being partly a novel compound useful as a vasodilator, etc., by formylating an amino group of a 2-carboxyaniline derivative, followed by ring closure in the presence of an amine or after converting a carboxyl group to carbodiimide group.
CONSTITUTION: An amino group of a compound shown by the formula I (R1 and R3 are lower alkyl; R2 is alkoxycarbonyl and R1WR3 are linked at 3W5 positions or 4W6 positions based on NH2) is formylated, and subjected to ring closure in the presence of an amine shown by the formula II [R4 is a group shown by the formula III or IV (R5WR7 are H or halogen; R6 is CF3, etc.; R7 is CN, etc.; R8 is H or lower alkyl], or subjected to ring closure after a carboxyl group shown by the formula I is converted to carbodiimide by the amine shown by the formula II and the amino group is formylated. The reaction product is optionally hydrolyzed to give advantageously a compound shown by the formula I being partly a novel compound useful as a vasodilator, improver for blood stream, antihypertensive agent or agent for arterioschlerosis.
EGUCHI MASAO
TANAKA HIROMICHI
ITOU SHIGERU
TAKASHIMA YOSHIMI
KOBAYASHI MASAHIKO
Next Patent: HETEROCYCLIC DERIVATIVE* ITS MANUFACTURE AND MEDICINAL COMPOSITION CONTAINING IT