反应详情

To a solution of (4-{4-[5-(6-trifluoromethyl-pyridin-3-ylamino)-pyrazin-2-yl]-phenyl}-cyclohexyl)-acetic acid methyl ester (0.051 g) in 4 Ml THF/water (1:1) was added solid lithium hydroxide (0.030 g). The reaction was stirred at room temperature for 48 h. then heated to 45° C. for 24 h. The reaction was neutralized with 6 N hydrochloric acid and then purified by reverse-phase preparative HPLC to afford the title compound: 1H NMR (400 MHz, DMSO-D6) δ ppm 1.1 (s, 2H) 1.3 (s, 1H) 1.6 (s, 2H) 1.9 (s, 6H) 3.5 (s, 6H) 7.4 (s, 2H) 7.9 (s, 1H) 8.0 (s, 2H) 8.6 (s, 1H), 8.6 (s, 1H) 8.9 (s, 1H) 9.1 (s, 1H) 10.9 (s, 1H); (M+H)+457.1.

1. temperaturethen heated to 45° C. for 24 h
2. custompurified by reverse-phase preparative HPLC