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Synthesis of 4′-iodo-4′-[14-14C]-deoxydoxorubicin hydrochloride (FCE 21954)

✍ Scribed by Erminia Fontana; Antonino Suarato; Michele Caruso; Gian Piero Vicario

Publisher
John Wiley and Sons
Year
1988
Tongue
French
Weight
242 KB
Volume
25
Category
Article
ISSN
0022-2135

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✦ Synopsis

The synthesis of 4' -iodo-4 l -[ 14-l4C1 -deoxydoxorubicin hydrochloride (PCE 21954) in five steps is described. 4 -Epi-N-trif luoroacetyl-[ 14-14C] -daunorubicin has been employed as starting material. substitution of C-4l-OH with iodine and subsequent hydroxylation of the side chain, via the 14-bromo derivative, of 41-iodo-41 -[ 14-14Cl-deoxydaunorubicin afforded the final product, in an overall radiochemical yield of 20%, 96% radiochemically pure and with a specific radioactivity of 252 MBq/mol (6.8 mCi/mmol).

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