Process for the preparation of benzoic acid derivatives...

Details Process for the preparation of benzoic acid derivatives... Process for the preparation of benzoic acid derivatives...

C - Chemistry, Metallurgy

07

C

167/254, 167/262

C07C 65/01 (2006.01) A01N 37/36 (2006.01) A01N 39/00 (2006.01) A61K 31/235 (2006.01) C07C 33/20 (2006.01) C07C 65/21 (2006.01) C07C 69/78 (2006.01) C07C 69/92 (2006.01) C07C 205/19 (2006.01) C07C 205/37 (2006.01)

Patent

CA 1254226

ABSTRACT OF THE DISCLOSURE This invention concerns a process for the preparation of benzoic acid derivatives with the general formula: Image (I) in which: A represents a straight or branched alkyl chain with 5 to 7 carbon atoms, X represents the oxygen atom or a direct bond, R represents hydrogen or an alkyl group with 2 to 6 carbon atoms, possibly substituted by an alcohol function, with the proviso that if R is H and A is a neopentyl group, X is a direct bond, and the salts of the said derivatives. The compounds possess antimicrobial activity. This process consists of: (1) subjecting the compound of formula IV to catalytic hydrogenation: Image (IV) in which X and A are as defined above to form the corresponding aniline derivatives, (2) the addition, to the said aniline derivatives, of sodium nitrite in acidic medium, to form the corres- ponding diazoniums, (3) the conversion of the said diazoniums to benzonitriles by the action of cuprous cyanide, (4) the conversion of the benzonitriles obtained to formula I compounds and (5) if necessary, convert the said compound obtained to a pharmaceutically acceptable salt.

461069

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