Réaction #1536359

ord-234f52a0e8fa4171a906792a71f101a4

Conditions de réaction

Conditions détaillées
See reaction.notes.procedure_details.

Traitement

  1. 1
    AutreAt 125° C.
  2. 2
    Températureis maintained at this temperature for five hours
  3. 3
    FiltrationThe difficultly soluble trimethoprim hydrochloride is filtered off
  4. 4
    Concentrationthe filtrate is concentrated in vacuo
  5. 5
    AutreUpon recrystallization from ethanol

Mode opératoire

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.

Source

DOI: 10.6084/m9.figshare.5104873.v1Brevet: US04189581uspto-grants-1980_02