AI Article Synopsis
- A new method is introduced for creating 3'-fluorinated nucleoside analogues using aminocatalytic fluorination of 2'-ketonucleosides that are easy to handle.
- The technique was initially aimed at producing 3'-fluoroguanosine (3'-FG), a component of the anticancer drug MK-1454, but has since been adapted to develop various 3'-fluoronucleosides.
- This approach highlights the potential of 2'-ketonucleosides as a versatile foundation for further innovation in nucleoside analogues, suggesting broad applications in drug discovery.
Article Abstract
Herein, we present a strategy for the preparation of 3'-fluorinated nucleoside analogues the aminocatalytic, electrophilic fluorination of readily accessible and bench-stable 2'-ketonucleosides. Initially developed to facilitate the manufacture of 3'-fluoroguanosine (3'-FG)─a substructure of anticancer therapeutic MK-1454─this strategy has been extended to the synthesis of a variety of 3'-fluoronucleosides. Finally, we demonstrate the utility of the 2'-ketonucleoside synthon as a platform for further diversification and suggest that this methodology should be broadly applicable to the discovery of novel nucleoside analogues.
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| http://dx.doi.org/10.1021/acs.orglett.2c03367 | DOI Listing |
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