4.7 Article

Catalytic Direct α-Amination of Arylacetic Acid Synthons with Anilines

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JOURNAL OF ORGANIC CHEMISTRY
卷 85, 期 20, 页码 13363-13374

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.0c02122

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  1. DST [DST/INSPIRE/04/2015/002248]
  2. CSIR (CSMCRI) [MLP 0028]
  3. UGC

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A unique alpha-amination approach using various anilines has been developed for arylacetic acids via adaptation as benzazoles. The reaction proceeds through a single electron transfer mechanism utilizing an iron-based catalyst system to access alpha-(N-arylamino)acetic acid equivalents. Modification of approved drugs, facile cleavage of the benzazole auxiliary, and tolerance of amide linkage forming conditions constitute the potential applicability of this strategy.

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