通过1,3-偶极环加成反应合成3-吡咯螺环氧化吲哚的研究进展

Research Progress of Synthesis of Pyrrolo Spirooxindoles via 1,3-dipolar Cycloaddition

作为一种重要的天然生物碱,吡咯螺环氧化吲哚骨架一直是天然产物化学和药物化学领域里的研究热点。由于含吡咯螺环氧化吲哚骨架分子广泛具有抗氧化、抗肿瘤等生物活性,近年来对其进行全合成和衍生化合成研究也持续升温。以各种取代的氨基酸为原料和各种取代羰基原位产生亚胺叶立德,然后再和α,β-不饱和烯烃发生1,3-偶极[3+2]环加成反应是合成各种吡咯螺环氧化吲哚类化合物的一种有效方法。本文对这一合成方法在近几年的研究进展进行了综述。

As an important functional group,the pyrrolo spirooxindole skeleton has always been a hot topic of ongoing interests,both in the natural products and in therapeutic agents.In recent years,tremendous interest has been devoted to the preparation of pyrrolo spirooxindoles due to their varied biological activities including antioxidant,antibacterial,and insecticidal behavior.The synthetic method of pyrrolo spirooxindoles via 1,3 -dipolar cycloaddition of in situ azomethine ylides,is an powerful process in many real drug synthetic applications.This review summarized recent progress on this synthetic method of pyrrolo spirooxindoles via 1,3-dipolar cycloaddition of in situ azomethine ylides.