Department of Chemical Sciences, Tezpur University , Napaam, Tezpur, Assam 784028, India.
Central Research Facility, Indian Institute of Technology Kharagpur , Kharagpur 721302, India.
J Org Chem. 2017 Feb 17;82(4):2193-2198. doi: 10.1021/acs.joc.6b02378. Epub 2017 Jan 27.
The present work reports a Pd/Ag-promoted amidoalkylation reaction involving various γ-hydroxy lactams and C/O/S nucleophiles at room temperature. The dual mode of activation of both the electrophile and nucleophile by in situ generated catalytically active cationic Pd species facilitates the reaction at room temperature. Among the synthesized isoindoline derivatives, three compounds are found to be active against vancomycin and methicillin-resistant S. aureus strain with appreciable MIC values.
本工作报道了一种 Pd/Ag 促进的酰胺烷基化反应，涉及各种 γ-羟基内酰胺和 C/O/S 亲核试剂，在室温下进行。通过原位生成的催化活性阳离子 Pd 物种对亲电试剂和亲核试剂的双重活化模式促进了室温下的反应。在所合成的异吲哚啉衍生物中，有三种化合物对万古霉素和耐甲氧西林金黄色葡萄球菌菌株表现出活性，MIC 值相当可观。
