ES325019A1 - A procedure for the preparation of heterociclic compounds. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

A process for the preparation of heterocyclic compounds, of the general formula ** (See formula) ** where Z represents one of the groups ** (See formula) ** R1, R2 and R3 are each hydrogen, halogen, lower alkyl or lower alkoxy, R4 and R5 are, individually, hydrogen, lower alkyl or benzyl, wherein at least one of the symbols R4 and R5 is hydrogen, or either R4 and R5, taken together with the nitrogen atom, are a monoheterocyclic ring structure that includes at most one other heteroatom, chosen in the group consisting of nitrogen and oxygen, and which carries at most one single substituent in the nucleus of the heterocyclic ring, R6 is hydrogen or lower alkyl, R7 is hydrogen, lower alkyl, phenyl or halophenyl, R8 is hydrogen, lower alkyl or lower carboxyalkyl, R9 is hydrogen, lower alkyl or lower alkanoyloxy, n is an integer per value from 2 to 6, A is a carbonyl group or a methylene group and B is a thio group, a sulfinyl group or a sulfonyl group, and its acid addition salts with pharmaceutically acceptable acids, which consists in reacting a compound of the general formula wherein R1, R2, R3, R6, R7, A, B and Z have the meaning set forth above, with a compound of the general formula ** (See formula) ** or first with a compound of the general formula ** (See formula) ** and then with an amine of the general formula ** (See formula) ** (in formulas III, IV and V above, R4, R5 and n have the meaning already stated, X is Hal or a sulfonyloxy group and Hal is chlorine, bromine or iodine), and converting, if desired, a carbonyl group of the resulting product into a methylene group, in oxidizing, if desired, a thio group, in introducing, if desired, a lower alkanoyloxy group as a substituent R9 and in converting, if desired , in a salt of acid addition a resulting base. (Machine-translation by Google Translate, not legally binding)