Process for the manufacture of phenylacetic acid derivatives

Details Process for the manufacture of phenylacetic acid derivatives Process for the manufacture of phenylacetic acid derivatives

C - Chemistry, Metallurgy

07

C

C07C 51/12 (2006.01) C07D 413/12 (2006.01) C07D 213/75 (2006.01) C07D 239/48 (2006.01)

Patent

CA 2437501

The present invention relates to a process for the manufacture of compounds of general formula (I), wherein R2a, R2b are, independently from each other, hydrogen; halogen; lower alkoxy; cyano; -COOH; lower alkoxycarbonyl; or lower alkyl, optionally substituted by halogen; and R3a, R3b are, independently from each other, hydrogen; lower alkyl; lower cycloalkyl or, if taken together, - (CH2)n with n=2,3 or 5. The compounds of formula (I) are valuable intermediates for the manufacture of therapeutically active compounds such as 2-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl- pyridin-3-yl)-isobutyramide and 2-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-N- (2-morpholin-4-yl-4-o-tolyloxy-pyrimidin-5-yl)-isobutyramide.

La présente invention concerne un procédé de production de composés correspondant à la formule générale (I), dans laquelle: R?2a¿, R?2b¿ représentent, indépendamment l'un de l'autre, hydrogène, halogène, alcoxy inférieur, cyano, -COOH, alcoxycarbonyle inférieur ou alkyle inférieur, éventuellement substitué par halogène; et R?3a¿, R?3b¿ représentent, indépendamment l'un de l'autre, hydrogène, alkyle inférieur, cycloalkyle inférieur ou bien, ensemble, -(CH¿2?)¿n?- où n = 2, 3 ou 5. Lesdits composés correspondant à la formule (I) constituent des intermédiaires appréciables pour la préparation de composés thérapeutiquement actifs tels que le 2-(3-5-bis-trifluorométhylphényl)-N-méthyl-N-(6-morpholin-4-yl-4-yl-4-o-tolylpyridin-3-yl)-isoburyramide et le 2-(3-5-bis-trifluorométhylphényl)-N-méthyl-N-(2-morpholin-4-yl-4-o-tolyloxy-pyrimidin-5-yl)-isobutyramide.

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