Hydrochloric Acid → HCID 86712737, compound

Participants

Reaction Steps

Ammonium carbonate (903 mg 9.40 mmol) was added to a suspension of 2-(2-(2-(2-((1-(1-(tert-butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)ethyl)phenyl)acetic acid (A136) (270 mg, 0.470 mmol), HOBt (317 mg, 2.35 mmol) and EDCl.HCl (450 mg, 2.35 mmol) in Et3N (1.0 mL) and DMF (25 mL) and the resulting solution was stirred at 40° C. overnight. The volatiles were removed in vacuo and the resulting residue was dissolved in EtOAc (250 mL) and washed with water (250 mL). The organics were adsorbed onto silica gel and the product was purified by silica gel column chromatography (Biotage Isolera, 40 g SiO2 cartridge, 0-100% EtOAc in petroleum benzine 40-60° C., then 0-20% MeOH in EtOAc) to yield the title compound (A137) as a white solid (171 mg, 63%). LCMS-A: rt 6.481 min; m/z 574.3 [M+H]+.

Provenance & Evidence