反应详情

To a solution of methyl ((8R)-8-{[(4-fluorophenyl)sulfonyl]amino}-6,7,8,9-tetrahydropyrido[3,2-b]indolizin-5-yl)acetate (0.46 g, 1.1 mmol) in DMF (5.5 mL) was added at 0° C. under nitrogen 60% NaH in oil (0.04 g, 1.2 mmol, 1.1 equiv.). After a period of 10 min., methyl iodide (0.076 mL, 1.2 mmol, 1.1 equiv.) was added and the reaction mixture aged 1 h at room temperature. The reaction mixture was poured over 25% aqueous ammonium acetate solution and ethyl acetate. The organic phase was separated, dried over sodium sulfate, filtered and evaporated under reduced pressure. The residue was purified by combiflash (hexane to 100% ethyl acetate) to provide 420 mg of the title compound.

1. waitthe reaction mixture aged 1 h at room temperature
2. customThe organic phase was separated
3. dry with materialdried over sodium sulfate
4. filtrationfiltered
5. customevaporated under reduced pressure
6. customThe residue was purified by combiflash (hexane to 100% ethyl acetate)