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目的优化白内障药物法可林1的合成工艺,以用于工业化生产。方法以O-苯二胺为起始原料,经缩合反应、磺化反应制得目标产物法可林1。结果对反应物配比、催化剂选择、反应温度及时间等因素进行了优化研究,使得该合成反应条件温和,后处理简单,总收率达40.7%,文献收率为24.8%。结论结构经~1H-NMR、MS确证,优化后的工艺更适合工业化生产。
Objective To optimize the synthesis of cataract drugs Falkolin 1 for industrial production. Methods O-phenylenediamine as the starting material, the condensation reaction, the sulfonation reaction of the target product Farkolin 1. Results The factors such as the ratio of reactants, the choice of catalysts, the reaction temperature and the time were optimized. The results showed that the reaction conditions were mild and the post-treatment was simple. The total yield was 40.7% and the yield of literature was 24.8%. Conclusion The structure of ~ 1H-NMR, MS confirmed that the optimized process is more suitable for industrial production.