Mannich反应合成新型氮杂环取代岩白菜素衍生物

Synthesis of Novel N-Hetercycle Substitued Bergenin Derivatives by Mannich Reaction

岩白菜素分别与四氢吡咯和哌啶经Mannich反应,合成得到2个新的氮杂环取代岩白菜素衍生物(2a,2b)。考察了溶剂、温度和时间等因素对反应的影响。在优化反应条件下,2a和2b的合成收率分别为48%和44%。

Two novel N-hetercycle substituted derivatives were synthesized by Mannich reaction of Bergenin with formaldehyde and pyrrolidine or piperidine. The effects of reaction conditions including solvent, temperature, and reaction time were evaluated. Under the optimal reaction conditions, the yields of 2a and 2b were up to 48% and 44%, respectively.