Background: Onychine is a 4-azafluorenone alkaloid isolated from the Annonaceae family, in low concentrations. Onychine and its analogs exhibit a wide range of pharmacological activities such as antifungal, antibacterial, anticancer, and antimalarial. Because of the high bioactivity of some 4-azafluorenone derivatives, several synthetic methods have been developed for their procurement.

Objective: Considering the importance of these alkaloids, we aim to present the main synthetic approaches to onychines and its derivatives and the biological activity of some 4-azafluorenones.

Methods: The most prominent methodologies for the synthesis of onychines were reviewed.

Results: In this work, we cover many synthetic approaches for the synthesis of onychine and 4-azafluorenone derivatives including intramolecular cyclizations, multicomponent reactions, microwave-assisted multicomponent reactions, Diels-alder reactions, among others. Moreover, we also review the biological activity of 4-azafluorenones.

Conclusion: 4-azafluorenones have risen as prominent structures in medicinal chemistry; however, most of the time, access to new derivatives involves toxic catalysts, harsh reaction conditions, and long-step procedures. Therefore, the development of new synthetic routes with more operational simplicity, simple purification procedure, good yields, and low environmental impact, is desirable.

背景：Onychine是从番荔枝科家族中分离得到的低浓度的4-氮杂芴酮生物碱。Onychine及其类似物表现出广泛的药理活性，例如抗真菌，抗菌，抗癌和抗疟疾。由于某些4-氮杂芴酮衍生物具有很高的生物活性，因此开发了几种合成方法来进行采购。

目的：考虑到这些生物碱的重要性，我们的目的是提出主要的合成方法，包括甲y及其衍生物以及某些4-氮杂芴酮的生物活性。

方法：综述了合成y药的最主要方法。

结果：在这项工作中，我们涵盖了许多合成Onychine和4-氮杂芴酮衍生物的合成方法，包括分子内环化，多组分反应，微波辅助多组分反应，Diels-alder反应等。此外，我们还审查了4-氮杂芴酮的生物活性。

结论：4-氮杂芴酮已作为药物化学中的突出结构而出现。但是，在大多数情况下，获得新衍生物的过程涉及有毒催化剂，苛刻的反应条件和长期步骤。因此，需要开发具有更多操作简便性，纯化步骤简单，产率高且对环境影响小的新合成路线。