反应详情

To a solution of 3-(4′,5′-difluoro-2′-methoxy-biphenyl-4-yloxymethyl)-benzoyl chloride (10 g, 25.7 mmol), triethylamine (10 mL, 64 mmol) in anhydrous THF (50 mL) was added in portions of tert-butylglycine methyl ester at 0° C., followed by slowly warming up to room temperature overnight while stirring. The mixture was diluted with EtOAc, washed with water and brine, dried over sodium sulfate, filtered and evaporated. The oily residue was purified by column (0-30% EtOAc in hexane) to give {[3-(4′,5′-difluoro-2′-methoxy-biphenyl-4-yloxymethyl)-benzoyl]-tert-butyl-amino}-acetic acid ethyl ester, 11.6 g (91%). LC-MS (ES) calculated for C28H29F2NO5, 497; found m/z 498 [M+H]+.

1. washwashed with water and brine
2. dry with materialdried over sodium sulfate
3. filtrationfiltered
4. customevaporated
5. customThe oily residue was purified by column (0-30% EtOAc in hexane)