Barroso, Santiago; Joksch, Markus; Puylaert, Pim; Tin, Sergey; Bell, Stephen J.; Donnellan, Luke; Duguid, Stewart; Muir, Colin; Zhao, Peichao; Farina, Vittorio; Tran, Duc N.; de Vries, Johannes G. published the artcile< Improvement in the Palladium-Catalyzed Miyaura Borylation Reaction by Optimization of the Base: Scope and Mechanistic Study>, Synthetic Route of 329214-79-1, the main research area is palladium catalyzed Miyaura borylation aryl halide base optimization; Arylboronic acid ester preparation.
Aryl boronic acids and esters are important building blocks in API synthesis. Pd-catalyzed Suzuki Miyaura borylation is the most common method for their preparation This paper describes an improvement of the current reaction conditions. By using lipophilic bases such as K 2-Et hexanoate, borylation reaction could be achieved at 35° in <2 h with very low Pd loading (0.5 mol %). A preliminary mechanistic study shows a hitherto unrecognized inhibitory effect by the carboxylate anion on the catalytic cycle, whereas 2-Et hexanoate minimizes this inhibitory effect. This improved methodol. enables borylation of a wide range of substrates under mild conditions. Journal of Organic Chemistry published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Synthetic Route of 329214-79-1.