ES417136A1 - Procedure for the obtaining of new derivatives of acids trumodous aminobencenocarboxilicos. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure for obtaining new derivatives of triiodinated aminobenzenecarboxylic acids, of general formula **(See formula)** where A means a hydrogen atom, a carboxyl group or the group (see formula), R1 means hydrogen, an alkyl or alkenyl residue with a maximum of 4 carbon atoms, an alkoxy residue with a maximum of 6 carbon atoms, a benzyl or phenyl residue, R2 means an alkyl or alkenyl residue or the -R6-COOH residue, or the R1 and R2 residues, together with the nitrogen atom, form a morpholino, piperidino or pyrrolidino ring, R3 signifies hydrogen, an alkyl residue with a maximum of 4 carbon atoms or an alkylene acid residue -carboxylic with a maximum of 4 carbon atoms, R4 signifies hydrogen or a lower alkyl radical, R5 means an alkyl or alkenyl radical with a maximum of 4 carbon atoms, an alkoxyalkyl radical with a maximum of 6 carbon atoms, a radical benzyl or phenyl, or R4 and R5 together with nitrogen form a pyrrolidino, piperidino or morpholino ring, and R6 means a straight chain or branched alkylene moiety with a maximum of 5 carbon atoms, where in the case that R2 represents the lower alkyl or lower alkylene moiety, either A means the carboxyl group or R3 the residue of alkylenecarboxylic acid, its lower alkyl esters or its pharmaceutically compatible salts, characterized in that derivatives of triiodinated aminobenzenecarboxylic acids of general formula **(See formula)** are reacted with compounds of the general formula **(See formula)** where, in formula II, Y means a halogen atom or the remainder (see formula), A'means a hydrogen atom, a carboxyl group, a carboxyl group esterified by aliphatic alcohols, an acid chloride group or the group (see formula), where R8 signifies a lower alkyl or alkenyl residue, the residues R6.COOH or R6COO alkyl, or R8 together with R1 and N, form a morpholino, piperidino or pyrrolidino residue, and in formulas II and III one of residues X'and X''is defined as hydrogen, the other as residue -COR9, where R9 means hydrogen, an alkyl residue with a maximum of 4 carbon atoms, an alkylenecarboxylic acid residue with a maximum of 4 carbon atoms, or a lower alkyl alkylenecarboxylate residue, where the acid component contains a maximum of 4 carbon atoms, being in formulas II and III R1, R4, R5 and R6 defined as in formula I and, in the case that R8 means a lower alkyl or alkenyl moiety, either A'means a carboxyl group or its alkyl ester or R9 means an alkyl moiety substituted by a carboxy or carboalkoxy group, with at least 1 mole of pentavalent phosphorus halides, preferably in an organic solvent indifferent in the compues cough obtained or in their hydrochlorides, the acid chloride groups existing in the aromatic nucleus are then reacted with amines of the formula **(See formula)** where R1 and R8 have the definition above and existing ester groups, if desired, are saponified, just as existing acidic or basic groups are transformed into salts, or acids or bases are released from such acids. (Machine-translation by Google Translate, not legally binding)