反应详情

Using the conditions of General Procedure C for Suzuki Coupling and Hydrolysis in Parallel Mode, 2-bromo-5-[4-(3,4-dichloro-phenyl)-thiazol-2-yl]-benzoic acid methyl ester (which may be prepared as described for Intermediate 6; 111 mg, 0.25 mmol) was reacted with 2-chloro-5-methylphenylboronic acid (available from Combi-Blocks Inc.; 85 mg, 0.5 mmol). The resulting ester was hydrolyzed and the acid was purified to give 2′-chloro-4-[4-(3,4-dichloro-phenyl)-thiazol-2-yl]-5′-methyl-biphenyl-2-carboxylic acid (59 mg, 50%). 1H NMR (400 MHz, DMSO-d6) δ 13.00 (br s, 3H), 8.51 (d, J=2.0 Hz, 1H), 8.48 (s, 1H), 8.34 (d, J=2.0 Hz, 1H), 8.27 (dd, J=8.0, 2.0 Hz, 1H), 8.09 (dd, J=8.5, 2.0 Hz, 1H), 7.77 (d, J=8.1 Hz, 1H), 7.44 (d, J=8.0 Hz, 1H), 7.38 (d, J=8.0 Hz, 1H), 7.19-7.24 (m, 1H), 7.18 (s, 1H), 2.34 (s, 3H).

1. customthe acid was purified