胡璧, 周则卫, 叶云鹏, 田原, 刘正明. 有机锗倍半氧化物类化合物的合成J. 药学学报, 1999, 34(11): 818-821.
引用本文: 胡璧, 周则卫, 叶云鹏, 田原, 刘正明. 有机锗倍半氧化物类化合物的合成J. 药学学报, 1999, 34(11): 818-821.
Hu Bi, Zhou Zewei, Ye Yunpeng Tian Yuan , Liu Zhengming, . SYNTHESIS OF ORGANIC GERMANIUM SESQUIOXIDEJ. Acta Pharmaceutica Sinica, 1999, 34(11): 818-821.
Citation: Hu Bi, Zhou Zewei, Ye Yunpeng Tian Yuan , Liu Zhengming, . SYNTHESIS OF ORGANIC GERMANIUM SESQUIOXIDEJ. Acta Pharmaceutica Sinica, 1999, 34(11): 818-821.

有机锗倍半氧化物类化合物的合成

SYNTHESIS OF ORGANIC GERMANIUM SESQUIOXIDE

  • 摘要: 目的:为寻找新型低毒有效放射增敏剂,合成了3 种类型有机锗倍半氧化物。方法:取代桂皮酸或取代苯丙炔酸与三氯锗仿反应,所得加成物经水解即得锗倍半氧化物;三氯锗基丙酰氯与亮氨酸乙酯或苯丙氨酸乙酯反应,所得产物水解即得N-(β-倍半氧锗基丙酰) 氨基酸酯。结果:合成的8个化合物中,7个(2 ~8) 为新化合物,羧基-β-( 取代苯基)乙烯基锗倍半氧化物为新类型化合物。结论:离体和整体实验结果表明,化合物4 有较显著的放射增敏作用,为新型低毒有效放射增敏剂。

     

    Abstract: AIM: To search for more effective and less toxic new type radiosensitizer, three types of organic germanium sesquioxide were synthesized. METHODS: 1. Substituted cinnamic acid or substituted phenyl propynoic acid reacted with trichlorogermane to afford the addition products which were hydrolyzed to the corresponding germanium sesquioxide. 2. β trichlorogermyl propionyl chloride reacted with ethyl ester of leucine or phenyl alanine to give the products which were hydrolyzed to the corresponding germanium sesquioxide. RESULTS: Eight germanium sesquioxides were synthesized and seven of them are new compounds (2~8). The type of carboxy -β-(substituted phenyl) vinyl germanium is reported for the first time. The structures of the compounds have been elucidated by UV, IR,1HNMR and elemental analysis. CONCLUSION: The synthetic compounds were tested for radiosensitizing activity, compound 4 exhibited significant radiosensitizing effect both in vitro and in vivo. Compound 4 showed great potential as a new type radiosensitizer with more effective action and lower toxicity.

     

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