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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

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【作者】 林木荣廖联安

【Author】 LIN Mu-rong, LIAO Lian-an (Dept. of Chem.,Xiamen Univ.,Xiamen 361005,China)

【机构】 厦门大学化学系!福建厦门361005

【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.

  • 【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
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