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为了从肉桂酸硫酯衍生物中寻找更有效的辐射损伤防护药,改变对羟基肉桂酸和芥子酸的结构,由4'-乙氧羰基-氧基苯丙烯酸酰氯和二乙胺基代乙硫醇,在碱催化下缩合,合成了4'-乙氧羰基-氧基-2—氯代苯丙烯酸二乙胺基代乙硫醇酯盐酸盐,以及3、4、5-三甲氧基苯丙烯酸二乙胺基代乙硫醇酯盐酸盐,经小鼠整体辐射后,早期给药试验证明:小鼠经60Coγ射线7.5~8.0Gy照射,30d存活率治疗组比对照组提高30%。还报道了化合物的质谱、红外及核磁共振光谱,讨论了有关化合物的ESR光谱。
In order to find a more effective radiation damage protective drug from thioester derivatives of cinnamic acid and to change the structure of p-hydroxycinnamic acid and sinapic acid, the structure of 4’-ethoxycarbonyl-oxybenzeneacrylic acid chloride and diethylaminoethanethiocarb Alcohol, condensation in the base catalysis, synthesis of 4’-ethoxycarbonyl-oxy-2-chlorophenyl acrylic acid diethylamino ethyl ethanethiol ester hydrochloride, and 3,4,5-trimethoxybenzene After the mice were irradiated by diets as a whole, the early administration experiments showed that mice irradiated by 60Coγ-ray 7.5 ~ 8.0Gy and the survival rate of 30d were higher than that of the control group 30%. The chemical, infrared and nuclear magnetic resonance spectra of the compounds were also reported. The ESR spectra of the compounds were also discussed.