N-(2-(5-溴-1H-吲唑-1-基)苯基)-2-氯烟酰胺的合成工艺研究

Study on Synthesis Technology of N-(2-(5-bromo-1H-indazol-1-yl)phenyl)-2-chloronicotinamide

采用单因素试验法对N-(2-(5-溴-1H-吲唑-1-基)苯基)-2-氯烟酰胺合成反应的反应条件进行了优化和研究,对关键步骤中间体I的合成确定了各个因素的最佳取值:反应时间为22h;物料配比应为5-溴吲唑:邻硝基氯苯:碳酸钾=1:0.85:1.15;反应温度为120℃;碱为碳酸铯。大大的提高了目标产物的总收率,为以后的大批量生产提供了有效途径。

In this paper,the reaction conditions of N-(2-(5-bromo-1H-indazol-1-yl)phenyl)-2-chloronicotinamide synthesis reaction were optimized and studied by single factor test,The optimum reaction time of each factor was determined for the synthesis of intermediate step I:reaction time was22h;the material ratio should be5-bromoindazole:o-nitrochlorobenzene:potassium carbonate=1:0.85:1.15;The temperature is120°C;the base is cesium carbonate.Greatly improving the total yield of the target product,for the future mass production provides an effective way.