PROCESS FOR THE MANUFACTURE OF ACYLQUINOLINE-3- CARBOXYLIC ACID DERIVATIVES

摘要

Process for the manufacture of acylquinoline-3-carboxylic acid derivatives Quinolinone derivatives of the formula (I) < IMG > (I), in which X represents oxy or a direct bond, R1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical or hydrogen, Ph represents an optionally additionally substituted 1,2phenylene radical containing the group R1-X-C(O)-, and one of the radicals R2 and R3 represents an optionally esterified or amidated carboxy group R4 and the other represents hydrogen or an aliphatic radical or, in the case of a radical R3, hydroxy, and in which either RA and RB together represent oxo, RC and RD to-gether represent an additional bond, or, when R2 represents a radical R4, RC is hydrogen and R3 and RD together represent oxo, and RE represents a radical R5 which represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or heterocyclic-aliphatic radical, or RA represents an optionally etherified hydroxy group and RB together with RC and also RD together with RE represent an additional bond in each case, or, when R2 represents a radical R4, RB and RC to-gether represent an additional bond and R3 and RD together represent oxo and RE represents a radical R5, and their salts, have antiallergic properties. They are manufactured, for example, by subjecting a compound of the formula (IV) < IMG > (IV) in which Z represents a removable radical, or a tautomer and/or salt thereof, to intramolecular cyclisation. The compounds of formula I are useful as antiallergics.