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用相应的取代苯甲醛(2)与β-苯胺基丙腈(3)在甲醇钠存在下,于二甲基亚砜液中缩合为2-取代苄基3-苯胺基丙烯腈(4),在甲醇钠催化下与盐酸胍反应生成2,4-二氨基-5-取代苄基嘧啶类化合物(1)。测定了12个化合物的抑菌活性,未发现活性优于 TMP 的化合物
The corresponding substituted benzaldehyde (2) and β-anilinopropionitrile (3) are condensed into 2-substituted benzyl 3-anilinoacrylonitrile (4) in dimethylsulfoxide solution in the presence of sodium methoxide. In sodium methoxide catalytic reaction with guanidine hydrochloride 2,4-diamino-5-substituted benzyl pyrimidine compounds (1). The antibacterial activities of 12 compounds were determined. No compounds were found to be more active than TMP