反应详情

NaH (810 mg, 32.1 mmol) was added to a solution of intermediate 2 (9.4 g, 21.4 mmol) in dry DMF. Then, iodomethane (3.64 g, 25.7 mmol) was added at room temperature. After 12 h, the reaction mixture was partitioned between water (pH 6) and AcOEt. Organic layer was dried over anhydrous Na2SO4, filtered and then evaporated. The residue was purified by silica column chromatography (gradient heptane/AcOEt 1:0 to 80:20) to yield 7.8 g (80%) of methyl 2-[2-(benzyloxy)phenyl]-3-cyclohexyl-1-methyl-1H-indole-6-carboxylate 3: m/z=454 (M+H)+.

1. customthe reaction mixture was partitioned between water (pH 6) and AcOEt
2. dry with materialOrganic layer was dried over anhydrous Na2SO4
3. filtrationfiltered
4. customevaporated
5. customThe residue was purified by silica column chromatography (gradient heptane/AcOEt 1:0 to 80:20)