Synthesis of Pyrrolo[2,3-c]azepine-4,8-dione Derivatives
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TQ465.91

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    Abstract:

    3-(1H-pyrrole-2-carbonyl)propionic acids (2a ~ 2c) were synthesized, in yields of 84.7 % ~ 91.2 %, by alkylations of methyl 3-(1H-pyrrole-2-carbonyl)aminopropionate (3) with alkyl halides and followed by hydrolyzation; the title compounds, 1a ~ 1c, were obtained via cyclizations of the acids (2a ~ 2c) in the presence of polyphosphoric acid and diphosphorus pentoxide, in yields of 69.1 % ~ 77.2 %. The overall yields of the three step reactions were 61.8 % ~ 69.1 %. And the α-glucosidase inhibitions of the three title compounds have also been studied.

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History
  • Received:December 09,2011
  • Revised:March 09,2012
  • Adopted:March 25,2012
  • Online: June 13,2012
  • Published:
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