N-苯基硫脲衍生物新的合成方法

Synthesis of N-Phenylthiourea Derivatives

硫脲衍生物是一类具有强烈生理和药理活性的有机试剂。以乙酰乙酰苯胺和硫氰酸铵为原料,在无催化剂的条件下,开发了一种合成标题化合物的方法。结果表明,乙酰乙酰苯胺无论是具有吸电子取代基还是给电子取代基,反应都可以顺利进行。合成了11种硫脲衍生物,所得产物的分离产率为81%~94%,并利用质谱、核磁共振波谱、红外光谱对所合成的化合物进行了表征。

Thiourea derivatives are a class of organic reagents possessing important biological and pharmaceutical activities.In this work,a catalyst-free method for the synthesis of N-phenylthiourea derivatives was developed directly from acetoacetanilides and ammonium thiocyanate.Investigation of representative acetoacetanilides demonstrates that the transformation is feasible whether the substituents are electron-donating or electron-withdrawing groups. The desired N-phenylthiourea derivatives were obtained with81% ~ 94% isolated yields and confirmed by MS,NMR and IR.