ANALOGIFORFARANDE FOR FRAMSTELLNING AV 2-AMINO-4HYDROXI-7,7-DIMETYL-7,8-DIHYDROPTERIDIN-6-KARBOXALDEHYD

摘要

Title compds are formula (I), where R' and R2 are 1-4C alkyl or CR1R2 is a 4-6 membered spiralkyl gp., and are prepd. e.g. by (a) mild oxidation (O2 and I2/H+) of the corresp. 6-hydroxymethyl deriv. or (b) reductive cyclisation of a 2-amino 4-(1,1'-dialkyl-3'-hydroxyacetonyl )amino 6-hydroxy 5-nitro-pyrimidine oxime. (I) inhibits hydroxymethyldihydropteridine pyrophosphokinase, and compsns. with dihydrofolate reductase inhibitors and/or p-aminobenzoic acid competitors are synergistic.