微波辅助合成金丝桃素四磺酸衍生物

利用微波辅助合成的方法,对金丝桃素四磺酸衍生物合成路线中的大黄素蒽酮缩合反应分别从微波加热温度、辐射时间和催化剂3个因素进行了优化,确定了最佳反应条件:温度150℃,反应时间1 h,不使用催化剂;该步反应的产率可达82.2%,整个合成路线经放大后的总产率为65.3%。与常规加热方法相比,微波辅助合成法提高了反应效率和产率,减少了副反应的发生,使合成工艺更加低碳环保。

Microwave assisted synthesis of tetrasulfonic acid hypericin derivative

Abstract: In the synthetic route towards tetrasulfonic acid dereivative of hypericin, self-condensation reaction of emodin anthrone was prompted by means of the microwave assisted organic synthesis. Three influencing factors of this step such as the microwave heating temperature, irradiation time and catalyst were studied and the resulting optimal conditions were determined as follows: 150°C, 1 h and no catalyst used. The yield of this step was increased by 82.2% with microwave assisted synthesis, and the total yield of the scaled-up synthesis of hypericin tetrasulfonic acid was achieved 65.3%. In comparison with conventional heating method, it is demonstrated that the use of the microwave method has enhanced the reaction efficiency and yield, reduced side-reactions and made the synthetic procedure more beneficial to low-carbon and environmental protection.