反应详情

To a DMF solution of 4-[2-(2,4-diamino-7H-pyrrolo [2,3-d]pyrimidin-5-yl)ethyl]benzoic acid (1.52 g) and methyl ester of N(δ)-t-butyloxycarbonyl-L-ornithine (1.3 g) was added diethyl cyanophosphate (1.4 g). The mixture was stirred for one hour at room temperature in the presence of triethylamine (3.0 g). The reaction mixture was concentrated under reduced pressure. The concentrate was purified by column chromatography on silica gel (carrier: 30 g; chloroform:ethanol containing 1% ammonium=20:1-15:1) to afford methyl N(α)-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-N-(δ)-(t-butyloxycarbonyl)-L-ornithinate (2.30 g; yield 85%).

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. customThe concentrate was purified by column chromatography on silica gel (carrier: 30 g; chloroform:ethanol containing 1% ammonium=20:1-15:1)