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http://dx.doi.org/10.5012/bkcs.2012.33.1.128

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)
Publication Information
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.
Keywords
Spiro(2H-1-benzopyran-2,4-piperidine)-6-yl derivatives; Solid-phase parallel synthesis; Druglike benzopyran core skeleton;
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