5-(aminomethyl)-4-aryl thiophene-2-amine derivative and preparation method thereof

The invention discloses a 5-(aminomethyl)-4-aryl thiophene-2-amine derivative and a preparation method thereof. The preparation method comprises the steps that 3-aryl-substituted propargyl alcohol, N-protected amine, N-halogenated succinimide and thiourea or a thiourea derivative serve as raw materials and are subjected to a multi-step cascade reaction under the catalytic action of acid, and therefore, one-pot synthesis of 5-(aminomethyl)-4-aryl thiophene-2-amine derivative is realized. The preparation yield of 5-(aminomethyl)-4-aryl thiophene-2-amine ranges from 15% to 80%, the method has the advantages of being easy to operate, mild in condition, high in yield and the like, and a brand-new synthesis method is provided for the 5-(aminomethyl)-4-aryl thiophene-2-amine derivative. 本发明公开了一种5-(氨基甲基)-4-芳基噻吩-2-胺衍生物及其制备方法，该制备方法以3位芳基取代的炔丙醇、N保护的胺、N-卤代丁二酰亚胺、和硫脲或硫脲衍生物为原料，在酸催化作用下进行多步串联反应，从而实现5-(氨基甲基)-4-芳基噻吩-2-胺衍生物的一锅法合成。本发明的5-(氨基甲基)-4-芳基噻吩-2-胺的制备产率在15％～80％之间，具有操作简单、条件温和、产率高等优点，为5-(氨基甲基)-4-芳基噻吩-2-胺衍生物提供了一种全新的合成方法。