FORFARANDE FOR FRAMSTELLNING AV SUBSTITUERADE 2,4-DIAMINO-5-BENSYLPYRIMIDINER

摘要

Cpds. of the formula: Ar-CH2-C(CN)=CH-NR5R6 (I) (where Ar is phenyl (opt. subst.) and NR5R6 is an aliph., heterocyclic or aromatic amino group in which one of R5 and R6 can be H) substantially free of contamination by the isomeric beta-amino-alpha-benzylidene-propionitriles are claimed; processes for their manufacture are also claimed. 2,4-Diamino-5-benzyl-pyrimidines (e.g. trimethoprim) having antimalarial and antibacterial activity are prepd. by reacting (I) with guanidine. Hydrolysis of (I) with aqs. acid gives new (and claimed) cpds. Ar-C(CN)=CH-OH, alkylation of which gives corr. beta-(lower alkoxy)-alpha-benzyl-acrylonitriles.