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

作　　者：林木荣[1] 廖联安[1] 

机构地区：[1]厦门大学化学系,福建厦门361005

出　　处：《厦门大学学报（自然科学版）》2000年第4期491-495,共5页Journal of Xiamen University：Natural Science

摘　　要：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.

关 键 词：溴莫普林 苄基嘧啶 KNOEVENAGEL缩合 抗菌药 

分 类 号：TQ463.54[化学工程—制药化工]