陈文彬, 王保钧, 陈宝珍, 章丽珠, 颜闵, 雷兴翰. 血吸虫病化学治疗的研究——ⅩⅪⅤ.5-2-(5-硝基呋喃基-2)-1-取代乙烯基-1,3,4-噁二唑酮及其1,3,4-噁二唑衍生物的合成J. 药学学报, 1986, 21(10): 761-766.
引用本文: 陈文彬, 王保钧, 陈宝珍, 章丽珠, 颜闵, 雷兴翰. 血吸虫病化学治疗的研究——ⅩⅪⅤ.5-2-(5-硝基呋喃基-2)-1-取代乙烯基-1,3,4-噁二唑酮及其1,3,4-噁二唑衍生物的合成J. 药学学报, 1986, 21(10): 761-766.
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CHEN Wen-Bin, WANG Bao-Jun, CHEN Bao-Zhen, ZHANG Li-Zhu, YAN Min , LEI Xing-Han, . CHEMOTHERAPEUTIC STUDIES ON SCHISTOSOMIASIS ⅩⅪⅤ. SYNTHESIS FOR DERIVATIVES OF 5-2-(5-NITRO-FURYI-2)-1-SUBSTITUTED VINYL-1, 3, 4-OXADIAZOL-2-ONE AND ITS 1, 3, 4-OXADIAZOLJ. Acta Pharmaceutica Sinica, 1986, 21(10): 761-766.
Citation: CHEN Wen-Bin, WANG Bao-Jun, CHEN Bao-Zhen, ZHANG Li-Zhu, YAN Min , LEI Xing-Han, . CHEMOTHERAPEUTIC STUDIES ON SCHISTOSOMIASIS ⅩⅪⅤ. SYNTHESIS FOR DERIVATIVES OF 5-2-(5-NITRO-FURYI-2)-1-SUBSTITUTED VINYL-1, 3, 4-OXADIAZOL-2-ONE AND ITS 1, 3, 4-OXADIAZOLJ. Acta Pharmaceutica Sinica, 1986, 21(10): 761-766.
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血吸虫病化学治疗的研究——ⅩⅪⅤ.5-2-(5-硝基呋喃基-2)-1-取代乙烯基-1,3,4-噁二唑酮及其1,3,4-噁二唑衍生物的合成

CHEMOTHERAPEUTIC STUDIES ON SCHISTOSOMIASIS ⅩⅪⅤ. SYNTHESIS FOR DERIVATIVES OF 5-2-(5-NITRO-FURYI-2)-1-SUBSTITUTED VINYL-1, 3, 4-OXADIAZOL-2-ONE AND ITS 1, 3, 4-OXADIAZOL

    摘要
  • 摘要: 本文报道硝基呋喃乙烯基-1,3,4-噁二唑及其酮类衍生物44个的合成。关键中间体α-取代β-(5-硝基呋喃基-2)丙烯酰彤魄仿照文献已知方法制备的,然后分别与光气或溴化腈作用生成相应的1,3,4-噁二唑衍生物Ⅰ,Ⅱ。经感染日本血吸虫病小白鼠的预防和治疗试验,发现化合物Ⅰ1具有显著的抗血吸虫作用,并试用于家犬的血吸虫病,证明有一定的疗效。但效果不及呋喃丙胺,故未作临床观察。

     

    Abstract: Forty-four compounds of nitrofuranvinyl-1,3,4-oxadiazol-2-one and its 1,3,4-oxadiazole have been synthesized. The key intermediate, α-substituted 5-nitro-2-furylacryloylhydrazine, was prepared by known method and it reacted subsequently with phosgen or bromocyanogen to form the corresponding 1,3,4-oxadiazolone of compound Ⅰ and Ⅱ respectively.

     

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