Abstract
AbstractThe preparation of estromustine (EoM), estramustine (EaM) and estramustine phosphate (EMP) specifically labelled with deuterium is reported. A two‐step, one‐pot procedure based on the reaction of N,N‐bis(2‐chloroethyl)carbamoyl chloride with the commercially available [2,4,16,16‐2H4]estrone (1) or [2,4,16,16,17‐2H5]estradiol (2) afforded [2,4,16,16‐2H4]estromustine (3) and [2,4,16,16,17‐2H5]estramustine (4), respectively. The phosphorylation of 4 followed by hydrolysis gave [2,4,16,16,17‐2H5]estramustine phosphate (5) in 65% chemical yield from 2. Copyright © 2004 John Wiley & Sons, Ltd.
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