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A set of pyrimidine nucleosides fused with a 4'-,3'--propylene bridge was successfully synthesised in 12 steps from 1,2:5,6-di--isopropylidene-α-d-glucofuranose, an inexpensive starting material, based on a ring-closing metathesis (RCM) reaction followed by Vorbrüggen-type nucleobase coupling. Antiviral and cytotoxicity activities of the targeted modified nucleosides, as well as their phosphoramidate prodrugs, are described.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8459888 | PMC |
| http://dx.doi.org/10.1002/ejoc.201100859 | DOI Listing |
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