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Synthesis of estromustine, estramustine and estramustine phosphate labelled with deuterium

✍ Scribed by Danilo Giribone; Erminia Fontana

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
93 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

The 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, H 4 ]estrone (1) or [2,4,16,16, H 5 ]estradiol (2) afforded [2,4,16, H 4 ]estromustine (3) and [2,4,16,16, H 5 ]estramustine (4), respectively. The phosphorylation of 4 followed by hydrolysis gave [2,4,16,16, H 5 ]estramustine phosphate (5) in 65% chemical yield from 2.

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