Microwave-Assisted Silylation-Animation of Uracil Acyclonucleosides to 4-Alkylamino-2(lH)-Pyrimidinone Analogues

摘要

The synthesis of acyclic N~4-substituted cytosine nucleo-side phosphonates using a microwave-assisted N~4-silylation-amina-tion and olefin cross-metathesis as key assembly steps is described. The microwave-assisted silylation-amination is compared to a conventional heating protocol. While yields and purities of the coupling products were comparable under both conditions, microwave heating allows a significant acceleration of the reaction (from 48 h to 5 h).