反应详情

To methyl 2-(3-(4-hydroxyphenyl)isoxazole-5-carboxamido)-3-methylbutanoate (200 mg) in N,N′-Dimethyl formamide (4 ml), cesium carbonate (245 mg) was added and stirred for 15-20 minutes. To this 2-chloro-6-fluorobenzo[d]thiazole (141 mg) was added and the reaction mixture was stirred at RT for 18 hours. Solvent was evaporated to obtain pale brown solid, which was purified by column chromatography (silica gel, EtOAc—CHCl3) to obtain off white solid, which was crystallized using DCM-Petroleum ether to obtain the title compound as white solid. Yield: 240 mg (81%); MS (ES+): m/z 470 (M+1); 1HNMR (DMSO-d6, 300 MHz): δ 9.27 (d, 1H), 8.08 (d, 2H), 7.93 (dd, 1H), 7.8 (s, 1H), 7.74 (dd, 1H), 7.67 (d, 2H), 7.31 (m, 1H), 4.33 (m, 1H), 3.69 (s, 3H), 2.23 (m, 1H), 0.98 (d, 6H).

1. stirringthe reaction mixture was stirred at RT for 18 hours
2. customSolvent was evaporated
3. customto obtain pale brown solid, which
4. customwas purified by column chromatography (silica gel, EtOAc—CHCl3)
5. customto obtain off white solid, which
6. customwas crystallized