title: Synthesis of a Nucleobase-Modified ProTide Library.
abstract: A new method for the construction of (aryloxy)phosphoramidate nucleoside prodrugs is presented. An (aryloxy)phosphoramidate ribose derivative as key building block was used for coupling with a number of nucleobases under Vorbrüggen reaction conditions yielding the protected ProTides in excellent yields. Selective hydrolysis of the acetoxy groups on the sugar moiety afforded a series of the desired ProTides. The advantage of this approach, when compared to classical procedures, is the greater flexibility for achieving structural variety of the nucleobase moiety.
authors: KU Leuven , Rega Institute for Medical Research, Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium.
authors: Ling-Jie
authors: LJ
authors: Gao
authors: KU Leuven , Rega Institute for Medical Research, Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium.
authors: Steven De
authors: S
authors: Jonghe
authors: KU Leuven , Rega Institute for Medical Research, Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium.
authors: Piet
authors: P
authors: Herdewijn