An Efficient Synthesis of 2-Hydroxyethyl N,N,N',N'-Tetrakis(2-chloroethyl)phosphorodiamidate

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• 作者：R. Jason Herr ; Paul Zhichkin ; Pedro E. Hern&aacute ; ndez-Abad ; Harold Meckler ; and Steven R. Schow
• 刊名：Organic Process Research & Development
• 出版年：2001
• 出版时间：July 2001
• 年：2001
• 卷：5
• 期：4
• 页码：442 - 444
• 全文大小：40K
• 年卷期：v.5,no.4(July 2001)
• ISSN：1520-586X

文摘

A process for the multikilogram preparation of 2-hydroxyethylN,N,N',N'-tetrakis(2-chloroethyl)phosphorodiamidate has beenachieved in substantially pure form by a short syntheticsequence starting from phosphorus oxychloride and 2 equiv ofbis(2-chloroethyl)amine. This process involves a two-step preparation of the intermediate mustard chloride in one pot, followedby the base-catalyzed reaction with excess ethylene glycol. Thismethod has been carried out to provide 2.9 kg of this key drugsubstance intermediate in 52% overall yield.