Solid-Phase Synthesis of Imidazo[1,2-a]pyridine Using Sodium Benzenesulfinate as a Traceless Linker
作者:Yu Chen、Yulin Lam、Yee-Hing Lai
DOI:10.1021/ol026797b
日期:2002.10.1
[formula: see text] The preparation of the first library of imidazo[1,2-a]pyridine derivatives on a solid support is described. A sulfone linker strategy was applied in the synthesis. Key steps involved in the solid-phase synthetic procedure include (i) alpha-haloketone resin formation by sulfinate-->sulfone alkylation, (ii) imidazo[1,2-a]pyridine ring formation by treatment with 2-aminopyridine, (iii)
描述了在固体载体上的咪唑并[1,2-a]吡啶衍生物的第一个文库的制备。在合成中采用了砜接头策略。固相合成过程中涉及的关键步骤包括(i)通过亚磺酸盐->砜烷基化形成α-卤代酮树脂,(ii)通过用2-氨基吡啶处理形成咪唑并[1,2-a]吡啶环,(iii )砜阴离子烷基化,以及(iv)通过氧化消除释放无痕产物。合成了12个咪唑并[1,2-a]吡啶的文库。