Synthesis And Structure Modification Of Steroids With Pyridine Rings

Steroid derivatives has a comprehensive application in pharmaceuti- cal field, it is the important aera of the drug production and research. The steroidal heterocycle always has biological activity and applied values. In order to find novel steroid compounds and explore the relationship between structure and biological activity, a series of steroids with pyridine ring were synthesized. The first part steroids and propargylamine were selected as the raw materials, which were catalyzed by Cu（NO₃）₂ through sequential amination, annulation, aromatization reaction. Nine compounds were obtained by colum chromatography and High-speed-Countercurrent Chromatography. The second part these compounds reacted with acylchloride in dichloromethane to afford other eleven new compounds, totally twenty new compounds were reported for the first time. The structure of all the compounds were confirmed by 1^H NMR、IR and MS, and two of them were determined by X-ray analysis. Five compounds were chosen to carry out the anti-tumor activity test.