[1,2]-Aryl migration in the synthesis of substituted indoles: scope, mechanism, and high throughput experimentation |
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Authors: | Tao Pei David M Tellers Eric C Streckfuss Cheng-yi Chen Ian W Davies |
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Institution: | Department of Process Research, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, United States |
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Abstract: | A mild regioselective synthesis of substituted indoles from readily accessible 1-(2-aminophenyl)-2-chloroethanones is described. Addition of a range of carbon nucleophiles to α-chloro acetophenones 1 generates 2-substituted indoles 2 in moderate to excellent yields. A reaction mechanism involving a 1,2]-aryl migration is proposed. This useful transformation is further examined using high throughput experimentation. |
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