反应详情

A mixture of (S)-4-(2-(2-carboxyacetoxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide (50 mg, 0.099 mmol), tert-butyl 2-(cyclopropylmethoxy)-4-(hydroxymethyl)phenyl-(methylsulfonyl)-carbamate (73 mg, 0.2 mmol), DMAP (14.5 mg, 0.12 mmol), and ECD (57 mg, 0.3 mmol) in DMF (1.5 ml) was stirred at RT overnight. The reaction mixture was quenched with water, and the product was extracted with EtOAc. The organic phase was washed with HCl 1M, NaHCO3 sat. sol. and brine. The organic layer was dried over Na2SO4 and evaporated to dryness. The crude (70 mg) was used for the next step without any further purification.

1. customThe reaction mixture was quenched with water
2. extractionthe product was extracted with EtOAc
3. washThe organic phase was washed with HCl 1M, NaHCO3 sat. sol. and brine
4. dry with materialThe organic layer was dried over Na2SO4
5. customevaporated to dryness
6. customThe crude (70 mg) was used for the next step without any further purification