N-cyclopropylation of indoles and cyclic amides with copper(II) reagent |
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| Authors: | Tsuritani Takayuki Strotman Neil A Yamamoto Yuhei Kawasaki Masashi Yasuda Nobuyoshi Mase Toshiaki |
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| Affiliation: | Process Research, PreClinical Department, Banyu Pharmaceutical Co. Ltd., 3 Okubo, Tsukuba, Ibaraki, Japan. takayuki_tsuritani@merck.com |
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| Abstract: | Copper-mediated coupling reactions of cyclopropylboronic acid with indoles and cyclic amides are described. The process utilizes catalytic or stoichiometric amounts of copper(II) acetate, DMAP, and NaHMDS at 95 degrees C under an atmosphere containing oxygen. A variety of functional groups remain intact throughout the reaction. |
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