Pertusati F, McGuigan C
School of Pharmacy and Pharmaceutical Sciences, Redwood Building, King Edwards VII Avenue, CF10 3NB, Cardiff, Wales, UK.
Chem Commun (Camb). 2015 May 11;51(38):8070-3. doi: 10.1039/c5cc00448a. Epub 2015 Apr 13.
The first copper-catalysed diastereoselective synthesis of P-chiral phosphoramidate prodrugs (ProTides) is reported. This procedure allows the synthesis of diastereomeric-enriched mixtures of ProTides. Application of this methodology to the asymmetric phosphorylation of purine and pyrimidine nucleoside analogues is presented.
报道了首例铜催化的P-手性磷酰胺酯前药(ProTides)的非对映选择性合成。该方法可用于合成富含非对映体的ProTides混合物。本文还介绍了该方法在嘌呤和嘧啶核苷类似物不对称磷酸化中的应用。