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）.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2014年第2期104-106,共3页
Chinese Journal of Pharmaceuticals
关键词
氨磷汀
细胞保护剂
合成
amifostine
cytoprotective agent
synthesis
