Catalytic direct amidations in tert-butyl acetate using B(OCH₂CF₃)₃.

ABSTRACT: Catalytic direct amidation reactions have been the focus of considerable recent research effort, due to the widespread use of amide formation processes in pharmaceutical synthesis. However, the vast majority of catalytic amidations are performed in non-polar solvents (aromatic hydrocarbons, ethers) which are typically undesirable from a sustainability perspective, and are often poor at solubilising polar carboxylic acid and amine substrates. As a consequence, most catalytic amidation protocols are unsuccessful when applied to polar and/or functionalised substrates of the kind commonly used in medicinal chemistry. In this paper we report a practical and useful catalytic direct amidation reaction using tert-butyl acetate as the reaction solvent. The use of an ester solvent offers improvement

SUBMITTER: Coomber CE 

PROVIDER: S-EPMC6724682 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature