Microwave-Assisted Silylation-Amination of Uracil Acyclonucleosides to 4-Alkylamino-2(1H)-Pyrimidinone Analogues

Abstract

The synthesis of acyclic N⁴-substituted cytosine nucleoside phosphonates using a microwave-assisted N⁴-silylation-amination 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).

Key words

microwaves - silylation-amination - olefin cross-metathesis­ - acyclic nucleoside phosphonates

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