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Synlett 1999; 1999(11): 1829-1831
DOI: 10.1055/s-1999-2938
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A New Method for the Synthesis of 5-Fluorouracil Prodrugs

Pascale Jolimaître* , Christiane André-Barres, Myriam Malet-Martino, Robert Martino, Isabelle Rico-Lattes
  • *Laboratoire des IMRCP (Groupe de RMN Biomédicale), UMR CNRS 5623, Université Paul Sabatier, 118 route de Narbonne, 31062 Toulouse, France; E-mail: rmnbio@ramses.ups-tlse.fr
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Publication History

Publication Date:
31 December 1999 (online)

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Bromo-tris(dimethylamino)-phosphonium-hexafluorophosphate (BROP) is a particularly suitable reagent for synthesising some 5-fluorouracil prodrugs in a one step reaction. Several acids, especially retinoic acid, were bound to the N1 of 5-fluorouracil, with yields of about 50% after purification.

N1-retinoyl-5-fluorouracil - BROP - artificial nucleosides - prodrug