Microwave‐Assisted One‐Step Synthesis of Acetophenones

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The regiochemistry of the palladium‐mediated arylation (Heck arylation) of enol ethers is sensitive to the structure of the enol ether, the arylating agent and the catalytic system. In this study, an effective and practical method was successfully developed for the synthesis of acetophenones with high regioselectivity under palladium‐catalyzed conditions. A variety of acetophenones was readily prepared from aryl iodides in good to excellent yields under microwave irradiation in a single step. The key feature of our new protocol is the use of vinyloxytrimethylsilane as a highly regioselective acylation reagent.

Document Type: Research Article

DOI: http://dx.doi.org/10.1002/adsc.201200334

Affiliations: 1: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, People's Republic of China, phone: (+86)-21-5080-7042, Fax: (+86)-21-5080-7042 2: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, People's Republic of China

Publication date: November 26, 2012

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