新苄基嘧啶类抗菌药溴莫普林的合成

Studies on the Synthesis of Brodimoprim,a New Antibacterial Benzylpyrimidine

４－溴－３， ５－二甲氧基苯甲醛（２）与 β－甲氧丙腈缩合得 ６１． ３％的（Ｚ）－肉桂腈（４ａ），４ａ经碱性催化１，３－质子转移异构化后与胍环合得６５．６％的澳莫普林（１）．（１）是一种具有广谱抗菌活性的新苄基嘧啶类抗菌药．

Synthesis of Brodimoprim was studied and the products was characterized by using NMR method. The results indicated that: The reaction of 4-bromo-3, 5-dimethoxybenzaldehyde (2) with β-methoxy-propanenitrile can give Z-cinnamonitrile (4a) with a yield of 61. 3%; the synthesis of (1 ) was accomplished by base-promoted condensation of 4a with guanidine (65. 6 % ). (1) is a new antibacterial benzylpyrimidine with a broad spectrum of antimicrobial activities.