GSK-A1及其衍生物的合成

Study on the Synthesis of GSK-A1 and Its Derivatives

设计了一条新的合成路线,以5-溴-2-甲氧基吡啶、吗啉、2-氟苯胺和联硼酸频那醇酯等为原料,经硝化、磺酰化、硼酸酯化和Suzuki-Miyaura等反应得到目标产物GSK-A1,总收率达到19.33%。并在该工艺基础上设计合成了9个新的衍生物,其结构经^(1)H NMR和HR-MS(ESI-TOF)确证。

A new synthetic route was designed,which took 5-bromo-2-methoxypyridine,morpholine,2-fluoroaniline and pinacol diboron as raw materials,and undergoes the reactions of nitration,sulfonylation,borate esterification,Suzuki-Miyaura and others.Then the target product GSK-A1 was obtained,and the total yield reached 19.33%.And on the basis of this process,nine new derivatives were designed and synthesized,and their structures were confirmed by^(1)H NMR and HR-MS(ESI-TOF).