Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Solid-phase Parallel Synthesis of a Novel N-[Alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted Amide and Amine Drug-like Libraries

  • Kim, Ji-Hye (Center for Innovative Drug Library Research, Department of Chemistry, Dongguk University) ;
  • Gong, Young-Dae (Center for Innovative Drug Library Research, Department of Chemistry, Dongguk University) ;
  • Lee, Gee-Hyung (Center for Innovative Drug Library Research, Department of Chemistry, Dongguk University) ;
  • Seo, Jin-Soo (Center for Drug Discovery Platform Technology, Korea Research Institute of Chemical Technology)
  • Received : 2011.11.01
  • Accepted : 2011.11.11
  • Published : 2012.01.20
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Abstract

We report the solid-phase library construction of 222 number of a novel N-[alkyl sulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B derivatives. The polymer-bound N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 9 and amine 10 derivatives were obtained by first diversity generation with various acid chlorides and alkyl halides. Further reactions on the resins 9 and 10 with substituted sulfonyl chlorides produced the desired N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B analogues.

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References

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