反应详情

2,2-Difluoro-2-fluorosulfonylacetic acid (205 μl, 1.98 mmol) in MeCN (20 ml) is added via a syringe pump to a mixture of N-(trans-4-trifluoromethyl-cyclohexyl)-2-(2-hydroxy-ethoxy)-6-amino-5-nitro-nicotinamide (390 mg, 0.994 mmol) and CuI (94 mg, 0.49 mmol) in MeCN (40 ml) over 2.5 h at 55° C. It is stirred for additional 20 min, then the mixture is concentrated and purified via extensive chromatography.

1. concentrationthe mixture is concentrated
2. custompurified via extensive chromatography