Wenlong Wei, Junbo Li, Xin Yang
Oct 28, 2008
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ChemInform
Abstract
The crystalline 4-ethyl-2,3-dioxopiperazine-1-carboxamido-p-hydroxyphenylacetyl chloride was prepared in 97.6% yield when triphosgene was reacted with p(-)-2-[(4-ethyl-2,3-dioxo-1-piperazineyl)-carbonylamino]-2-(4-hydroxyphenyl)acetic acid (HO-EPCP) in methylene dichloride at 0-5 "C in the presence of triethylamine (TEA). This new method without using chlorinating agent such as phosgene, diphosgene, phosphorus oxychloride or oxalyl chloride enjoys a number of advantages in that the reaction is carried out under mild conditions and is clean.