Homologation of Carboxylic Acids Using a Radical-Polar Conjunctive Reagent.

ABSTRACT: Homologations of organic molecules that add a carbon atom to the substrate are useful in drug discovery to access compounds with improved properties that otherwise present a synthetic challenge. Carboxylic acids are present in many bioactive molecules and are widely available building blocks for chemical synthesis, yet their direct homologation is unknown. This valuable transformation currently necessitates implementation of multistep processes that require the use of carboxylic acid derivatives rather than the native substrates, and commonly involves highly reactive and toxic reagents. Herein, we report the first one-step homologation directly from native carboxylic acids using a novel, bench-stable (1-phosphoryl)vinyl sulfonate reagent under mild conditions. This strategy was applied to

SUBMITTER: Gruhin JN 

PROVIDER: S-EPMC11758094 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature