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<p>The union of two powerful transformations, directed C–H activation and decarboxylative cross-coupling, for the
enantioselective synthesis of vicinally functionalized alkyl, carbocyclic, and heterocyclic compounds is described. Starting from
simple carboxylic acid building blocks, this modular sequence exploits the residual directing group to access more than 50 scaffolds
that would be otherwise extremely difficult to prepare. The tactical use of these two transformations accomplishes a formal vicinal
difunctionalization of carbon centers in a way that is modular and thus amenable to rapid diversity incorporation. A simplification of
routes to known preclinical drug candidates is presented along with the rapid diversification of an antimalarial compound series.
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