Simmons Bryan J, Weires Nicholas A, Dander Jacob E, Garg Neil K
Department of Chemistry and Biochemistry, University of California, Los Angeles, California 90095, United States.
ACS Catal. 2016 May 6;6(5):3176-3179. doi: 10.1021/acscatal.6b00793. Epub 2016 Apr 12.
We report the catalytic alkylation of amide derivatives, which relies on the use of nonprecious metal catalysis. Amide derivatives are treated with organozinc reagents, utilizing nickel catalysis, to yield ketone products. The methodology is performed at ambient temperature and is tolerant of variation in both coupling partners. A precursor to a nanomolar glucagon receptor modulator was synthesized using the methodology, underscoring the mild nature of this chemistry and its potential utility in pharmaceutical synthesis. These studies are expected to further promote the use of amides as synthetic building blocks.
我们报道了酰胺衍生物的催化烷基化反应，该反应依赖于非贵金属催化。酰胺衍生物与有机锌试剂在镍催化下反应，生成酮产物。该方法在室温下进行，并且对两种偶联试剂的变化具有耐受性。利用该方法合成了一种纳摩尔级胰高血糖素受体调节剂的前体，突出了这种化学方法的温和性质及其在药物合成中的潜在用途。这些研究有望进一步促进酰胺作为合成砌块的应用。
