Facile Synthesis of Thymidine Derivatives by Cross-Coupling of 5-Halogenouridine Derivatives with Trimethylaluminum
- 1 January 1993
- journal article
- research article
- Published by Georg Thieme Verlag KG in Synthesis
- Vol. 1993 (02) , 213-215
- https://doi.org/10.1055/s-1993-25833
Abstract
An efficient method for the introduction of a methyl group in the 5-position of uridine derivatives is described. This method involves three steps: protection of 5-halogenouridines 4 and 5 with hexamethyldisilazane, a palladium-catalyzed cross-coupling of the pertrimethylsilylated nucleosides with trimethylaluminum, and subsequent deprotection to afford the corresponding thymidine derivatives 6 in high overall yields.Keywords
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