PROCESS FOR PREPARATION OF SUBSTITUTED 3'-HYDROAZINO-DIPHENYL-3-CARBOXYLIC ACID COMPOUNDS

摘要

The present invention provides a process for the preparation of substituted 3′-hydrazino-biphenyl-3-carboxylic acid compounds. The present invention further provides a process for the preparation of 3′-{N′-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-pyrazol-4-ylidene]hydrazino}-2′-hydroxybiphenyl-3-carboxylic acid, its intermediate compounds and pharmaceutically acceptable salts thereof.

主权项

1. A process for the preparation of substituted 3′-hydrazino-biphenyl-3-carboxylic acid compounds of formula I and salts thereof,wherein R represents hydrogen (compound of formula Ia), linear or branched C1-6 alkyl (compound of formula Ib, when R is methyl), C3-8 cycloalkyl, optionally substituted benzyl, linear or branched alkylalkoxy, tetrahydrofuranyl, tetrahydropyranyl, methyloxybenzyl, trialklsilyl, acyl, or trityl; the process comprising:
a) reacting a compound of formula III,wherein R is as defined above, X is selected from the group consisting of Cl, Br, and I, with a compound of formula IV,wherein R′ represents boronic acid, boronic acid ester or halogen in the presence of a metal catalyst; and
(b) optionally, deprotecting the compound of formula 1.