利扎曲坦的合成

Synthesis of Rizatriptan

利扎曲坦是一种治疗偏头痛的有效药物,耐受性好,不良反应轻。综述利扎曲坦的有关合成方法,并对合成方法进行分析和评价。在早期的合成方法中,Fischer吲哚反应产率很低;在由碘代胺与酰基硅烷经Pd催化偶联反应中,需-78℃的低温反应条件。从4-氨基-1,2,4-三唑开始的利扎曲坦合成和经Pd催化的碘化苯胺与炔烃偶联合成利扎曲坦的反应路线较适合工业化大生产的需要。

Rizatriptan is an effective drug used in treating migraine with tolerable side effect. Overviewed the synthetic methods of rizatriptan, analyzed and evaluated these methods. In the earlier synthetic method, Fischer Indole reaction rate was lower. In palladiumcatalysed cross-coupling reaction of aniline iodide and N,N-Dimethyl butyryl silane, reaction condition was strict because of needed -78℃. From the beginning of4-amino-1,2,4-triazol synthetic route and by palladium-catalysed cross-coupling reaction of aniline iodide and alkynes alkynyl reaction route, they met the needs of industrial production.