Diisopropylethylamine → HCID 16037880, compound

Participants

Reaction Steps

A solution of 3-{[(3-amino-3-benzyltetrahydrofuran-2-yl)oxy]methyl}-5-[(methylsulfonyl)(propyl)amino]benzoic acid (25 mg, 0.04 mmol), 4-fluoro-R-alpha-methyl-benzyl amine (10 mg, 0.08 mmol), N,N-diisopropylethylamine (0.02 mL, 0.11 mmol), BOP reagent (25 mg, 0.06 mmol) in DMF (0.6 mL) is stirred at RT for 20 min and purified by preparative HPLC (5->95% CH3CN/H2O, 0.1% added TFA, C18 Sunfire Waters, 30×150 mm) to give 3-{[(3-amino-3-benzyltetrahydrofuran-2-yl)oxy]methyl}-N-[(1R)-1-(4-fluorophenyl)ethyl]-5-[(methylsulfonyl)(propyl)amino]benzamide (2 diastereoisomer separated). MS M+1=584.

Provenance & Evidence