METHOD OF PREPARING QUINOLINYL LACTAMS OR SALTS THEREOF

摘要

FIELD: chemical industry. SUBSTANCE: method of preparing new quinolinyl lactams of formula I: R1 wherein B is structure of formula I: wherein B is structure of general formula II: C3-C6 wherein Q is structure of formula III: R2 wherein CR4 is lower alkyl or saturated or unsaturated R4 carbocycle optionally substituted by halogen; is hydrogen or amino group; A is nitrogen or wherein is halogen or hydrogen; P is piperazinyl unsubstituted or substituted by lower alkyl or group of formula IV: wherein Hal is fluorine, chlorine, bromine or iodine, or salts thereof. Said method comprises reacting lactam compound B-OH wherein B is as defined above, in which functional hydroxyl and carboxyl groups are optionally protected, with phosgene at temperature from -80 C to about 0 C to form intermediate product of formula V: wherein B is as defined above, reacting the resulting intermediate product with compound of general formula HQ wherein Q is as defined above in which functional carboxyl group is optionally protected, subsequently removing protective groups and isolating the desired product in free state or as salt. EFFECT: new compounds have valuable properties. 8 cl, 3 ex