“一锅煮”法合成卢扎朵仑的研究

One-Pot Synthesis of Ruzadolane

为开发一种高效的反应体系合成卢扎朵仑,以卤代芳烃、DABCO和硫酚为原料,通过一种简单反应过程快速地将芳基、哌啶和硫酚等结构单元组装到复杂结构的卢扎朵仑上。该合成路线简洁、高效,原料廉价易得,适合工业化生产。

The development of an efficient reaction system to synthesize ruzadolane,a pharmacologically active compound as aromatic aminoalkyl thioether motif,has broad application prospects.Herein,we report a simple synthetic process to rapidly synthesize ruzadolane,where we made use of cheap and easily available aryl halide,DABCO and thiophenol as the starting materials.To yield complexes of ruzadolane with such important fragments as aryl groups,piperidine,and thioether can be efficiently taken place.This process can readily be expanded to the scale suitable for industrial manufacture.