反应详情

To a stirred solution of compound (S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((4-nitrophenoxy)-carbonyloxy)ethyl)pyridine 1-oxide, (227 mg, 0.388 mmol) in DCM (10 ml), (4-nitrophenyl)methanamine hydrochloride (88 mg, 0.465 mmol), and DMAP (56.9 mg, 0.465 mmol) were added. The reaction mixture was stirred at RT overnight. After 20 hours, the mixture was diluted with DCM and washed with a solution of K2CO3. he organic layer was dried over Na2SO4, evaporated and the resulting crude was purified by flash chromatography on silica gel (DCM:MeOH 10:0.3) affording the desired product (200 mg, 0.334 mmol, 86% yield, MS/ESI+ 598.3 [MH]+).

1. waitAfter 20 hours
2. washwashed with a solution of K2CO3
3. dry with materialhe organic layer was dried over Na2SO4
4. customevaporated
5. customthe resulting crude was purified by flash chromatography on silica gel (DCM:MeOH 10:0.3)