R. Herr, P. Zhichkin, †. P. E. Hernández-Abad
May 17, 2001
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0
Influential Citations
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Journal
Organic Process Research & Development
Abstract
A process for the multikilogram preparation of 2-hydroxyethyl N,N,N‘,N‘-tetrakis(2-chloroethyl)phosphorodiamidate has been achieved in substantially pure form by a short synthetic sequence starting from phosphorus oxychloride and 2 equiv of bis(2-chloroethyl)amine. This process involves a two-step preparation of the intermediate mustard chloride in one pot, followed by the base-catalyzed reaction with excess ethylene glycol. This method has been carried out to provide 2.9 kg of this key drug substance intermediate in 52% overall yield.