烟酰胺及其衍生物被认为是重要的药物中间体，一直是广泛化学修饰和严格药理学研究的焦点。在此，通过串联 CuAAC/环断裂/环化/氧化四组分反应程序，由 O-乙酰基肟、末端炔酮、磺酰叠氮化物和 NH4OAc 合成了一系列新型烟酰胺衍生物烟酰亚胺。该策略比之前报道的显着更有效，并且还测试了烟酰亚胺的细胞毒性。该项目不仅展示了用于创建烟酰亚胺的可持续且环保的多米诺骨牌方法，而且还为肝癌治疗提供了一种有前途的候选药物。该期刊版权所有©英国皇家化学学会。

Nicotinamide and its derivatives, recognized as crucial drug intermediates, have been a focal point of extensive chemical modifications and rigorous pharmacological studies. Herein, a series of novel nicotinamide derivatives, nicotinimidamides, were synthesized via a tandem CuAAC/ring-cleavage/cyclization/oxidation four-component reaction procedure from O-acetyl oximes, terminal ynones, sulfonyl azides, and NH4OAc. This strategy is significantly more efficient than previously reported, and the cytotoxicity of the nicotinimidamides is also tested. This project not only exhibits a sustainable and eco-friendly domino methodology for the creation of nicotinimidamides but also presents a promising candidate for liver cancer treatment.This journal is © The Royal Society of Chemistry.