反应详情

7.5 g of BOP are added to a mixture of 4.06 g of 2-(tert-butoxycarbonylamino)-3-(4-cyanophenyl)propionic acid and 1.15 ml of pyrrolidine in 20 ml of DMF, and the mixture is stirred for 2 hours at RT, while maintaining the pH at 7 by adding N-ethylmorpholine. The reaction mixture is concentrated under vacuum and the residue is chromatographed on silica gel, eluting with a chloroform/MeOH mixture (95/5; v/v). 3.8 g of the expected product are obtained.

1. temperaturewhile maintaining the pH at 7
2. concentrationThe reaction mixture is concentrated under vacuum
3. customthe residue is chromatographed on silica gel
4. washeluting with a chloroform/MeOH mixture (95/5; v/v)