含异噻唑的羧酸衍生物的合成研究

Synthesis of novel acid derivatives containing isothiazol

异噻唑类化合物在医药、农药和染料等领域有着重要作用,报道了一种含异噻唑的羧酸衍生物的新合成方法,以取代的苯甲酸、硫化钠和羟胺-O-磺酸等为原料,经缩合制备得到3个含异噻唑的羧酸衍生物。在该合成路线中,对反应原料中的羧基采取保护和脱保护的措施,经5步反应,得到标题化合物。标题化合物的结构经过1HNMR、MS等分析测试技术的确证。该合成路线反应条件温和、总产率较高,适于规模化合成。

Isothiazol derivatives take an important role in the synthetical reagent and pharmaceutical intermediates. Three novel acid derivatives containing isothiazol were synthesized. Starting from acetyl substituted benzoic acid and Na2S, the targeted compound was synthesized through a five-step proce- dures including the protection and deprotection of carhoxyl. The structure of the target compounds were confirmed by ^1HNMR and MS. The novel synthetic method has such advantages as mild condition and high yield. This method was suitable for industrial production.