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

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.