摘要
3-氨基丙醇与三氯氧磷环合制得2-氯四氢-2H-1,3,2-氧氮磷杂环己烯-2-氧化物,然后与2-氯乙胺盐酸盐进行烷基化反应,继而经氯乙酰氯酰化得3-(2-氯乙酰基)-2-[(2-氯乙基)氨基]四氢-2H-1,3,2-氧氮磷杂环己烯-2-氧化物,最后经硼氢化钠/浓硫酸还原得到抗肿瘤药异环磷酰胺,总收率为30%(以3-氨基丙醇计)。
Ifosfamide was synthesized from 3-aminopropanol by cyclization to give 2-chlorotetrahydro-2H- 1,3,2-oxazaphosphorine-2-oxide, which was alkylated with 2-chloroethylamine hydrochloride, acylated with chloroacetyl chloride, and then reduced by NaBH4/H2SO4 in 30 % overall yield.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2009年第7期483-485,共3页
Chinese Journal of Pharmaceuticals