反应详情

温度

0 °C

A mixture of 2-pyrrol-1-yl-ethanol (17 mg, 0.15 mmol) and NaH (5 mg, 60% dispersion in mineral oil, 0.13 mmol) in THF (200 μL) was stirred at 0° C. for 15 min. A solution of methyl 3-{[(5-chloro-3-methyl-1-benzothien-2-yl)sulfonyl]amino}benzoate (Example 74) (20 mg, 0.05 mmol) in THF (100 μL) was added, and the reaction mixture was stirred at 0° C. for another 6 h. The reaction was quenched by addition of cold MeOH and 4:1 water/HOAc (50 μL) before purified by preparative HPLC. The title compound was obtained in 53% yield (12.5 mg). MS (ESI+) m/z 475 [M+H]+.

1. stirringthe reaction mixture was stirred at 0° C. for another 6 h
2. customThe reaction was quenched by addition of cold MeOH and 4:1 water/HOAc (50 μL)
3. custombefore purified by preparative HPLC