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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 33, Number 1
BKCSDE 33(1)
January 20, 2012 

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
Ji-Hye Kim, Young-Dae Gong*, Gee-Hyung Lee, Jin-soo Seo
Spiro(2H-1-benzopyran-2,4-piperidine)-6-yl derivatives, Solid-phase parallel synthesis, Druglike benzopyran core skeleton
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.
128 - 136
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