PREPARATION OF NOVEL NITROGENNCONTAINING CONDENSED HETEROCYCLIC COMPOUND HAVING IMINO GROUP AT 22POSITION AND NITROGENNCONTAINING CONDENSED HETEROCYCLIC COMPOUND HAVING OXO GROUP AT 22POSITION CONTAIN

摘要

PURPOSE:To obtain the title compounds having anti-inflammatory, analgesic, and antiallergic actions, in high yield economically, by converting the imino group at the 2-position of a novel intermediate, obtained from 2-amino-benzthiazole and a piperazine derivative, into an oxo group. CONSTITUTION:A nitrogen-containing condensed heterocyclic compound of formula III (R1 is H, halogen, or halogen-substituted alkyl group; X1 is O or S) having an amino group at the 2-position and a piperazine derivative of formula IV (R2 is alkylene group; R3 is alkyl or hydroxyalkyl group; X2 is halogen) are heated in a suitable solvent to give a novel intermediate of formula I, which is heated or warmed in a suitable solvent to eliminate the imino group at the 2-position to give the objective compound of formula II having the oxo group. The compound of formula I has useful pharmacological actions on circulatory and nervous systems, and is a promising antibacterial.