氨磷汀的合成  

Synthesis of Amifostine

作　　者：杨益飞[1] 程惠[1] 韩静[1] 刘庆春[1] 孙建[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国医药工业杂志》2014年第2期104-106,共3页Chinese Journal of Pharmaceuticals

摘　　要：丙烯酰胺与乙醇胺加成生成3-[(2-羟乙基)氨基]丙酰胺,经硼氢化钠还原得重要中间体N-(2-羟乙基)-1,3-丙二胺,与浓盐酸成盐后,与氯化亚砜与DMF反应所得的Vilsmeier试剂进行氯代反应生成N-(2-氯乙基)-1,3-丙二胺二盐酸盐,最后与十二水硫代磷酸钠缩合得氨磷汀,总收率约54%(以丙烯酰胺计)。Amifostine was synthesized from acrylamide by addition with ethanolamine and reduction with sodium borohydride to give N-（2-hydroxyethyl）-1,3-propanediamine, which was subjected to salt formation and chlorination with Vilsmeier reagent prepared by SOC12 and DMF to afford N- （2-chloroethyl） -1,3-propanediamine dihydroehloride, followed by condensation with sodium thiophosphate dodecahydrate with an overall yield of about 54% （based on acrylamide）.

关 键 词：氨磷汀 细胞保护剂 合成 

分 类 号：R914[医药卫生—药物化学]