A procedure for the preparation of compounds given of anti-inflammatory properties. (Machine-translation by Google Translate, not legally binding)

摘要

A process for the preparation of compounds endowed with anti-inflammatory properties, of the formula: ** (See formula) ** where R1 and R2 are both selected from the group consisting of hydrogen, halogen, trifluoromethyl, (lower) alkyl, lower alkoxy, nitro, dialkyl (lower) amino, alkanoyl (lower), phenyl, phenoxy, lower alkyl phenoxy, halofenoxy benzyloxy, lower alkyl benzyloxy, lower alkoxy benzyloxy, halobenzyloxy; R3 is selected from the group consisting of hydrogen, lower alkyl and trifluoromethyl; R 4 is selected from the group consisting of hydrogen and lower alkyl; R5 is selected from the group consisting of hydrogen, lower alkyl, trifluoromethyl, lower alkenyl, and phenyl; R6 is selected from the radicals of the formula: ** (See formula) ** wherein R7 and R8 are both selected from the group consisting of hydrogen, halogen, trifluoromethyl, lower alkyl, lower alkoxy, lower alkylthio, trifluoromethyloxy, trifluoromethylthio, phenyl, phenoxy, halofenoxy, lower alkyl phenoxy, alkoxy (lower) phenoxy, phenylthio, nitro, benzyloxy and lower alkyl benzyloxy; and pharmacologically acceptable non-toxic salts thereof; whose process consists of acylating an indolyltetrazole of the formula: ** (See formula) ** wherein R1, R2, R3, R4 and R5 are those described above, preferably in the form of their alkali metal dimethyl salts, with an equimolar weight of approximately an acid halide of the formula: ** (See formula) ** wherein R6 is that described above and X is a halogen atom, or with a functional equivalent of said acid halide, in an inert organic solvent at a temperature comprised between about -20º C and about 50º C; and, if desired, by reacting the compound in which R1 or R2 is benzyloxy or nitro with hydrogen, in the presence of a catalyst, to produce the corresponding compound where R1 or R2 is hydroxy or amino respectively. (Machine-translation by Google Translate, not legally binding)