穿心莲内酯硝甲基衍生物的合成

Preparation of the nitromethylene substituted derivatives of andrographolide

目的合成穿心莲内酯硝甲基衍生物.方法利用Michael加成反应机理,将硝甲基基团引入到穿心莲内酯的分子结构中,再对其进行一系列的酯化反应.结果合成了16个新的穿心莲内酯硝甲基衍生物,这些新化合物的分子结构经核磁共振谱、质谱等数据确证.结论化合物Ⅰ1～Ⅰ16显示出不同的抗肿瘤活性.

Aim To search for vascular drugs from the andrographolide derivatives, the synthesis paths of the possible aim compounds were studied. Methods Nitro-group was led into the structure of andrographolide according to the mechanism of Michael addition. Then, the nitromethylene substituted intermediate was esterified by a series of different acids under different catalysts. Results A series of new nitromethylene substituted derivatives of andrographolide were synthesized, their structures were identified by ^1H-NMR and MS, and the preliminary anticancer activities were studied. Conclusion compounds I1-I16 show different antitumor activity.