10.1021/acs.joc.7b01355.s001 Alessandra Casnati Alessandra Casnati Raimondo Maggi Raimondo Maggi Giovanni Maestri Giovanni Maestri Nicola Della Ca’ Nicola Della Ca’ Elena Motti Elena Motti Pd-Catalyzed/Iodide-Promoted α‑Arylation of Ketones for the Regioselective Synthesis of Isocoumarins American Chemical Society 2017 Regioselective Synthesis reaction mixture iodide anions intramolecular cyclization process phosphine-free one-pot synthesis features access Arylation variety palladium-catalyzed α- arylation step 2- halobenzoates methodology Pd-Catalyzed 2- bromobenzoates selectivitie Isocoumarin antifungal activity group tolerance Xyridin Ketone yield ketone isocoumarin 2017-07-20 18:11:49 Journal contribution https://acs.figshare.com/articles/journal_contribution/Pd-Catalyzed_Iodide-Promoted_Arylation_of_Ketones_for_the_Regioselective_Synthesis_of_Isocoumarins/5229622 A variety of isocoumarins have been synthesized directly from 2-halobenzoates and ketones through a palladium-catalyzed α-arylation step followed by an intramolecular cyclization process. The addition of iodide anions to the reaction mixture increased yields and selectivities especially when 2-bromobenzoates were employed. This phosphine-free one-pot synthesis features a high functional group tolerance and gives access to richly decorated isocoumarins. This general methodology was successful in the total synthesis of Xyridin A, an important natural product with antibacterial and antifungal activity.