METHOD FOR THE PREPARATION OF COMPOUNDS WITH ANALGETIC AND ANTI-INFLAMMATORY ACTION AND METHOD FOR THE PREPARATION OF PHARMACEUTICAL PREPARATIONS CONTAINING THEM.

摘要

1387595 Derivatives of 4-aminoquinoline ROUSSEL UCLAF 10 April 1972 [8 April 1971] 16489/72 Heading C2C [Also in Division A5] The invention comprises compounds of formula and their non-toxic acid addition salts, wherein R 1 is H, F, Cl, Br, I, CF 3 , CN, NO 2 or C 1-8 alkyl, alkoxy, alkylthio, alkylsulphonyloxy, alkylamino or acylamino; R 2 is H, Cl or Me; Y is a thiophene or thiazole residue to which the amino and carboxylic group are attached in adjacent positions, which residue is optionally further substituted by C 1-6 alkyl; and X is H, C 1-6 alkyl, Ph, di(C 1-6 alkyl)amino-C 1-6 -alkyl (or a quaternary C 1-6 alkyl halide thereof), morpholinoalkyl, glyceryl (or a cyclic ketal thereof with Z 2 CO where Z is C 1-5 alkyl) or 2-Y- 1,3-dioxan-5-yl where Y is C 1-6 alkyl or monocyclic aryl. In examples, these compounds are prepared by (1) reacting a 4-chloroquinoline with NH 2 -[Y]-CO 2 X, (2) hydrolysing the above esters to obtain the acids, (3) transesterification, or (4) hydrolysing esters of 2,2-dimethyl-1,3- dioxolan-4-ylmethanol to the corresponding glycerol esters.