反应详情

5.8 g of 2,4-diamino-5-(3,4,5-trimethoxybenzyl)-pyrimidine (trimethoprim) are suspended in 58 ml of chlorobenzene. At 125° C., 1.55 g of phenylacetyl chloride are dripped in, and the whole is maintained at this temperature for five hours. The difficultly soluble trimethoprim hydrochloride is filtered off and the filtrate is concentrated in vacuo. Upon recrystallization from ethanol there is obtained 4-amino-2-phenylacetamido-5-(3,4,5-trimethoxybenzyl)-pyrimidine of melting point 181° to 183° C.

1. customAt 125° C.
2. temperatureis maintained at this temperature for five hours
3. filtrationThe difficultly soluble trimethoprim hydrochloride is filtered off
4. concentrationthe filtrate is concentrated in vacuo
5. customUpon recrystallization from ethanol