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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
【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.
【Abstract】 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】 合成;
溴莫普林;
苄基嘧啶;
Knoevenagel缩合;
异构化;
【Key words】 synthesis; brodimoprim; benzylpyrimidine; knoevenagel condensation; isomerization;
【Key words】 synthesis; brodimoprim; benzylpyrimidine; knoevenagel condensation; isomerization;
- 【文献出处】 厦门大学学报(自然科学版) ,JOURNAL OF XIAMEN UNIVERSITY(NATURAL SCIENCE) , 编辑部邮箱 ,2000年04期
- 【分类号】TQ463
- 【被引频次】6
- 【下载频次】109