新型吲唑衍生物1-乙酸-吲唑-3-羧酸的合成

Synthesis of A Novel Indazole Derivative 1-(carboxymethyl)-Indazole-3-carboxylic Acid

吲唑羧酸衍生物具有潜在的生物活性,同时具有多配位中心的特点,容易与金属离子形成单核或多核金属有机配合物。本文以1-氢吲唑-3-羧酸为起始原料,经酯化,取代以及水解反应,通过3步合成了一种全新的吲唑双羧酸配体。中间体及最终产物经核磁共振氢谱、碳谱以及质谱确定。本方法合成步骤简洁,反应条件温和易操作,且各步骤均可重结晶纯化,无需柱层析等复杂步骤,能够大量合成。

Indoxazole carboxylic acid derivatives have potential biological activities along with the characteristics of multiple coordination centers,which result in easily forming mononuclear or poly-nuclear organometallic complexes with metal ions.A novel ligand,1-(carboxymethyl)-indoxazole-3-carboxylic acid,was synthesized from 1-hydroindazole-3-carboxylic acid,by esterification,substitution and hydrolysis.The intermediates and final products were identified by ^(1)H NMR,^(13)C NMR and MS.This method is simple,mild and easy to operate.All the intermediates and products could be purified by recrystallization instead of column chromatography,and can be synthesized in large quantities.