反应详情

To a solution of crude (R)-3-(1H-Indol-3-yl)-2-(5-trimethylsilanylethynyl-thiophene-2-sulfonylamino)-propionic acid 115 (0.126 g, 0.282 mmol) in dichloromethane/methanol mixture (1:1, 10 mL) was added K2CO3 (0.047 g, 0.34 mmol) and allowed to stir for 60 minutes. The reaction mixture was then filtered and retentate washed with dichloromethane-methanol mixture. The combined filtrate was concentrated under reduced pressure and then purified using a SAX column to obtain (R)-2-(5-Ethynyl-thiophene-2-sulfonylamino)-3-(1H-indol-3-yl)-propionic acid 116 (52 mg, 49%). LC-MS (ES+) 375; (ES−) 373.

1. filtrationThe reaction mixture was then filtered
2. washretentate washed with dichloromethane-methanol mixture
3. concentrationThe combined filtrate was concentrated under reduced pressure
4. custompurified