四组分双环化反应合成双吡唑并[3,4-b]吡啶

Synthesis of Bispyrazolo[3,4-b]Pyridine by Four-Component Bicyclization Reaction

吡唑并[3,4-b]吡啶可用作HSP90抑制剂、FGFR激酶抑制剂、mGluR5正变构调节剂等.现有的合成方法存在容易爆炸、产率不高、时间过长的缺点.从3-芳基吡唑和二羟基芳酮出发,通过[3+2+1]双杂环化反应,一步合成了双吡唑并[3,4-b]吡啶.该反应操作安全,产率高,时间短.

Pyrazolo[3,4-b]pyridine can be used as HSP90 inhibitor,FGFR kinase inhibitor,mGluR5 positive allosteric regulator,etc.The existing synthesis method has the disadvantages of easy explosion,low yield and long time.Starting from 3-arylpyrazole and dihydroxyaromatic ketone,bispyrazolo[3,4-b]pyridine was synthesized in one step by[3+2+1]bisheterocyclization reaction.The reaction is safe in operation,high in yield and short in time.