Nitrogen-containing heterocycles were employed in different applications such as pharmaceuticals, organic materials, natural products, and mainly in bioactive molecules. Pyrrolopyrazine as a biologically active scaffold contains pyrrole and pyrazine rings. Compounds with this scaffold have widely exhibited different biological activities, such as antimicrobial, anti-inflammatory, antiviral, antifungal, antioxidant, antitumor, and kinase inhibitory. In addition, many pyrrolopyrazine derivatives have been isolated from plants, microbes, soil, marine life, and other sources. This review explained various synthetic routes for pyrrolopyrazine derivatives, including cyclization, ring annulation, cycloaddition, direct C-H arylation, and other methods. Besides, pyrrolopyrazines are classified into three chemical categories with two or three nitrogen atoms, indicating various biological activities. According to the findings, pyrrolo [1,2-a] pyrazine derivatives exhibited more antibacterial, antifungal, and antiviral activities, while 5H-pyrrolo [2,3-b] pyrazine derivatives showed more activity on kinase inhibition. However, studies show that the action mechanisms of pyrrolopyrazine derivatives are not clearly recognized. Moreover, despite the scaffold’s importance, there are only a few Structure-Activity Relationship (SAR) research on it. Therefore, the synthetic methods and biological activities of pyrrolopyrazine derivatives discussed in this paper will certainly help medicinal chemistry researchers design and synthesize new leads to treat various diseases.

含氮杂环被用于不同的应用，如药物、有机材料、天然产物，主要用于生物活性分子。作为生物活性支架的吡咯并吡嗪含有吡咯和吡嗪环。具有这种支架的化合物已广泛表现出不同的生物活性，如抗菌、抗炎、抗病毒、抗真菌、抗氧化、抗肿瘤和激酶抑制。此外，许多吡咯并吡嗪衍生物已从植物、微生物、土壤、海洋生物和其他来源中分离出来。该综述解释了吡咯并吡嗪衍生物的各种合成路线，包括环化、环化、环加成、直接 CH 芳基化等方法。此外，吡咯并吡嗪分为三个化学类别，具有两个或三个氮原子，表示各种生物活性。根据研究结果，吡咯[1,2-a ] 吡嗪衍生物表现出更多的抗菌、抗真菌和抗病毒活性，而 5H-吡咯并 [2,3- b ] 吡嗪衍生物表现出更多的激酶抑制活性。然而，研究表明吡咯并吡嗪衍生物的作用机制尚未明确。此外，尽管支架很重要，但关于它的构效关系（SAR）研究很少。因此，本文所讨论的吡咯并吡嗪衍生物的合成方法和生物活性必将有助于药物化学研究人员设计和合成治疗各种疾病的新线索。