Abstract
AbstractThe cover picture shows the single‐step direct transformations of inosine into C6‐functionalized nucleosides by base‐promoted or palladium‐catalyzed phosphonium couplings. Since the pioneering work by Fox et al. in 1958, the functionalization of nucleosides has been routinely carried out in a multi‐step sequence including protection, activation, functionalization, and deprotection. As the first direct bond formation through C–OH bond activation of tautomerizable heterocycles with PyBroP, this new, mild, efficient, chemoselective, and versatile phosphonium coupling methodology has solved a long‐standing synthetic challenge of a single‐step transformation in nucleoside chemistry. Details of the discovery, mechanism, scope, and application of this technology are presented in the Microreview by F.‐A. Kang et al. on p. 461 ff.
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