Alemán-Ponce de León Diego, Sánchez-Chávez Anahí C, Polindara-García Luis A
Instituto de Química , Universidad Nacional Autónoma de México, Ciudad Universitaria , Ciudad de México 04510 , México.
J Org Chem. 2019 Oct 18;84(20):12809-12834. doi: 10.1021/acs.joc.9b01436. Epub 2019 Aug 21.
The development of a novel protocol for the fast introduction of the picolinamide directing group in aliphatic ketones by using the ammonia-Ugi 4-CR reaction and the subsequent evaluation of the Pd-mediated γ-C(sp)-H bond activation is described. The methodology allows the efficient construction of a series of γ-arylated α-aminoamides bearing a congested carbon in two steps.
描述了一种通过使用氨-乌吉4组分反应在脂肪族酮中快速引入吡啶甲酰胺导向基团的新方案,以及随后对钯介导的γ-C(sp)-H键活化的评估。该方法能够分两步高效构建一系列在拥挤碳位带有γ-芳基化α-氨基酰胺的化合物。