The azaindole chemical scaffold is represented in many biologically active natural products and synthetic derivatives. Recently, this chemical scaffold yielded several therapeutic agents for a variety of diseases. Due to the interesting biochemical and biophysical properties of various isomeric azaindoles, numerous investigators have designed and implemented novel synthetic methods for azaindole core units in the past few decades. By using these novel strategies, a number of diversely substituted azaindoles including bioactive natural products, key intermediates and drug candidates have been produced. Herein, we have reviewed the novel synthetic strategies developed for azaindoles since 2011 and highlight their attractive reaction mechanisms, advantages and their limitations. This review may offer potential solutions to develop novel and facile methodologies for the azaindole derivatives of biological interest.

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由吡啶和吡咯结构单元合成氮杂吲哚的最新进展

氮杂吲哚化学支架存在于许多具有生物活性的天然产物和合成衍生物中。最近，这种化学支架产生了多种用于多种疾病的治疗剂。由于各种异构的氮杂吲哚的有趣的生化和生物物理特性，在过去的几十年中，许多研究人员已经设计并实施了用于氮杂吲哚核心单元的新颖合成方法。通过使用这些新颖的策略，已经生产了包括生物活性天然产物，关键中间体和候选药物在内的多种多样的氮杂吲哚。在此，我们回顾了自2011年以来针对氮杂吲哚开发的新型合成策略，并重点介绍了其有吸引力的反应机理，优点和局限性。