芸香宁碱及其衍生物的合成研究进展

Review on Synthesis of Graveolinine and Its Derivatives

芸香宁碱属于2-苯基喹啉类,是从华南地区芸香科植物中提取出来的生物碱,具有广泛的生理活性。其合成分为多步法和一步法。前者原料价格低廉,反应条件温和,但是周期较长,原子利用率不高;一步法具有路线短,原子利用率高的优点,但原料价格昂贵,不易获得,反应收率低。目前中间体法更加经济,更容易衍生化,适用于实验室。但随着合成方法学的发展和高效催化剂的发现,一步法也可使用廉价易得的原料,具有更广阔的发展空间。

Graveolinine belongs to the 2-phenyl quinolone compounds, which is isolated from Ruta graveolens L. in the south of China. It has showed comprehensive pharmacological activities. The main synthesis methods of graveolinine derivatives could be divided into the multi-steps and one-step methods. The multi-steps method has the advantages of low material price and mild reaction conditions. Hhowever, the preparation scheme is long and the atomic utilization rate is not high. The one-step method has the advantages of short route and high atomic utilization rate, but the materials are expensive or difficult to obtain, and the yield is low. At present, the multi-steps method is more economy, easier to derivatize, and suitable for using in laboratory. However, with the development of synthetic methodologies and the discovery of high-efficiency catalysts, the one-step method can also use cheap and commercial available materials, and it will have a great potential for future development.