反应详情

4-((S)-2-((S)-3-(3-(2-Aminoethylcarbamoyl)phenylsulfonyl)thiazolidine-2-carbonyloxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide hydrochloride (195 mg, 0.244 mmol), 3-formylbenzoic acid (110 mg, 0.733 mmol), DMAP (5.97 mg, 0.049 mmol) and EDC (141 mg, 0.733 mmol) were dissolved in DMF. The reaction was stirred at RT overnight to achieve completion. The reaction mixture was diluted with water, and the precipitate was washed with water, dissolved in DCM and extracted with water. The organic phase was dried over Na2SO4 and concentrated under vacuum to give 3,5-dichloro-4-((S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((S)-3-(3-(2-(3-formylbenzamido)ethylcarbamoyl)-phenylsulfonyl)thiazolidine-2-carbonyloxy)ethyl)pyridine 1-oxide (100 mg, 0.112 mmol, 45.8% yield).

1. washthe precipitate was washed with water
2. dissolutiondissolved in DCM
3. extractionextracted with water
4. dry with materialThe organic phase was dried over Na2SO4
5. concentrationconcentrated under vacuum