反应详情

A solution of 36.0 mg (0.0759 mmol) 4-{4-[(4-cyano-1H-pyrrole-2-carbonyl)-amino]-3-cyclohex-1-enyl-phenyl}-piperidine-1-carboxylic acid tert-butyl ester (as prepared in the previous step) in 5 mL CH2Cl2 was treated with 4 drops MeOH and 1 mL TFA and stirred at RT for 2 h. MeOH (5 mL) was added, and solvents were evaporated in vacuo. Purification of the residue by RP-HPLC (C18) with 10-80% CH3CN in 0.1% TFA/H2O over 30 min afforded 22.0 mg (59%) of the title compound as a white solid: Mass spectrum (ESI, m/z): Calcd. for C23H26N4O, 375.2 (M+H), found 375.2.

1. customsolvents were evaporated in vacuo
2. customPurification of the residue by RP-HPLC (C18) with 10-80% CH3CN in 0.1% TFA/H2O over 30 min