反应详情

Methansulfonyl chloride (0.2 mL, 2.46 mmol) is added to a solution of 5-(2-hydroxymethyl-pyridin-4-yloxy)-indole-1-carboxylic acid (3-trifluoromethylphenyl)-amide, Example 25-D, (700 mg, 1.64 mmol) and triethylamine (0.7 mL, 4.92 mmol) in DCM (50 mL) at rt. After 1 h the reaction is partitioned between DCM and saturated aqueous NaHCO3. Organic layer is removed, dried over anhydrous Na2SO4, concentrated and then separated via FCC (EtOAc/heptanes 2:4 to EtOAc/heptanes 9:1) to give the title compound. MS (ESI) m/z 506.0 (M+1).

1. customAfter 1 h the reaction is partitioned between DCM and saturated aqueous NaHCO3
2. customOrganic layer is removed
3. dry with materialdried over anhydrous Na2SO4
4. concentrationconcentrated
5. customseparated via FCC (EtOAc/heptanes 2:4 to EtOAc/heptanes 9:1)