Sustainable Ru(II)-Catalyzed ortho-C(sp2) –H Hydroxyalkylation of Phthalazinones Using Ethyl Glyoxalate: Access to α,α′-Arylcarboxy sec-Alcohols

Synthesis DOI: 10.1055/a-2114-5426 An operationally simple and expeditious protocol for Ru(II)-catalyzed ortho-C(sp2)–H hydroxyalkylation of phthalazinones using commercially available ethyl glyoxalate in 2-Me-THF is reported. This greener approach involves the imine nitrogen on the phthalazinones as a directing group to effect the regioselective hydroxyalkylation. Ample examples of biologically relevant hydroxyalkylated phthalazinones were prepared, and relevant controlled studies were performed to decipher the reaction mechanism. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text

Source: Synthesis - August 7, 2023 Category: Chemistry Authors: Ramkumar, Alagumalai Gandhi, Thirumanavelan Tags: special topic Source Type: research