Water → HCID 18426156, compound

Participants

Reaction Steps

A mixture of 1-[4-(chloroformyl)benzyl]-4-[[N-(3-(trifluoromethyl)benzoyl)glycyl]aminomethyl]piperidine (0.042 mmol) with 2-methoxyethylamine (3.8 mg, 0.050 mmol), a piperidinomethylpolystyrene (46 mg) and dichloromethane (1.5 mL) was stirred at room temperature for 17 hours. Water (0.020 mL) was then added to the mixture, and the resulting mixture was stirred for 30 minutes. Methanol (1 mL) was then added to the obtained mixture, and the resulting mixture was loaded onto a Varian™ SCX column and washed with methanol (10 mL). The obtained crude product was eluted with a 2 M methanol solution of NH3 and concentrated to thereby provide 1-[4-[N-(2-methoxyethyl)carbamoyl]benzyl]-4-[[N-(3-(trifluoromethyl)benzoyl)glycyl]aminomethyl]piperidine (Compd. No. 1612) (26.7 mg, 100%). The purity was determined by RPLC/MS (92%). ESI/MS m/e 535.2 (M++H, C27H33F3N4O4).

Provenance & Evidence