反应详情

Trifluoroacetic acid (1.0 mL, 13.0 mol) is added dropwise to a slurry of 2-[3-(S)-(5′-chloro-[2,2′]bithiophenyl-5-sulfonylamino)-2-oxo-pyrrolidin-1-ylmethyl]pyrrolo[3,2-c]pyridine-1-carboxylic acid tert-butyl ester (0.13 g, 0.22 mmol) in CH2Cl2 (2 mL) at 0° C. After 30 min. the ice bath is removed and the solution is stirred at room temperature for 4 h. The reaction mixture is concentrated to dryness and the crude product is purified by RP-HPLC eluting in a gradient of 10% CH3CN/H2O (0.1% TFA) to 100% CH3CN. The appropriate product fractions are lyophilized to provide the title compound as a white solid.

1. customAfter 30 min. the ice bath is removed
2. concentrationThe reaction mixture is concentrated to dryness
3. customthe crude product is purified by RP-HPLC
4. washeluting in a gradient of 10% CH3CN/H2O (0.1% TFA) to 100% CH3CN