| 摘要 |
Substituted pteridines of the general formula <FORM:0654512/IV (b)/1> wherein NHR1 is an amino acid amide of paraaminobenzoic acid, are prepared by reacting 2,4,5-triamino-6-hydropyrimidine or a tautomer thereof, e.g. 2,4,5-triamino-6-oxo-pyrimidine or 2-imino-4,5-diamino-6-oxo-pyrimidine, an alpha - halo - beta - alkoxy - propionaldehyde or an acetal thereof and an amino acid amide of para-aminobenzoic acid. The reaction may be carried out at a temperature of 20 DEG to 80 DEG C., preferably from 30 DEG to 60 DEG C. The reaction may be carried out in water, methanol, ethanol, propanol, acetic acid, dioxane or a mixture thereof. The preferred propionaldehydes and acetals are alpha-bromo- and alpha-chlorobeta - ethoxy - propionaldehydes, and alpha - bromo - beta - ethoxy - propionaldehyde diethyl acetal, dimethyl acetal and dibutyl acetal. Amino acid amides of para-amino-benzoic acid mentioned are para-aminobenzoyl-glutamic acid and polypeptides thereof such as para-amino-benzoylglutamylglutamic acid and para-aminobenzoylglutamylglutamylglutamic acid, and others having a plurality of peptid linkages made up of one or more of the various amino acids such as para-aminobenzoyl-glutamylglycylglutamic acid, and amides derived from para-aminobenzoic acid and glycine, aspartic acid, leucine, alanine, isovaline or cysteine. The salts and esters of these amino acid amides of para-aminobenzoic may also be used. In the examples, pteroylglutamic acid, pteroyl alpha glutamylglutamic acid and pteroyl-gamma-glutamylglutamic acid are prepared. The Specification as open to inspection under Sect. 91 refers to the preparation of compounds of the above general formula, where R1 is any aromatic radical, by the above method using a primary aromatic amine as the third reactant. Aromatic amines mentioned are aniline, ortho-, meta- and para-substituted aniline, and the amides of aminobenzoic acid including ortho-, meta- and para-aminobenzamide and other aliphatic and aromatic amides which may be formed by the reaction of an aminobenzoyl halide with an aliphatic or aromatic amine such as ethylamine, ethanolamine, ethylhexylamine or morpholine. This subject-matter does not appear in the Specification as accepted.
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