Stereoselective Approach for the Synthesis of Diverse 1'-Modified Carbanucleosides

Org Lett. 2023 Nov 24;25(46):8377-8381. doi: 10.1021/acs.orglett.3c03518. Epub 2023 Nov 10.

Abstract

We describe an efficient and stereoselective synthesis of 1'-substituted-β-carbocylic nucleosides 5 via gem-dichlorooxirane intermediate 7, which directly condensed with weak nucleophiles such as pyrimidines or purines. The formation of gem-dichlorooxirane 7 and direct nucleobase condensation exclusively proceeded in protic polar solvents like MeOH. This method provides a general and modular route for the late-stage diversification of 1'-modified nucleosides.