Phthalazin-1(2H)-one is a diazaheterobicycle found in a wide variety of synthetic molecules relevant to several branches of chemistry, including medicinal chemistry. The versatility of phthalazinone core in drug discovery has promoted the search for new synthetic methods to get access to differently substituted and functionalized derivatives. This review highlights the latest advances in synthesis of phthalazinone derivatives that have relevance to drug discovery processes, analyzing modifications of classical methodologies based on [4 + 2] two-component cyclocondensations as well as novel multicomponent approaches, mostly based on a [3 + 2+1] three-component strategy and very attractive not only because of its synthetic efficiency but also in the matter of environmental compatibility.

Phthalazin-1（2H）-one是一种重氮杂双环化合物，存在于与化学（包括药物化学）几个分支相关的多种合成分子中。酞嗪酮核心在药物开发中的多功能性促进了寻找新的合成方法以获取不同取代和功能化衍生物的途径。这篇综述重点介绍了与药物发现过程有关的酞菁酮衍生物合成的最新进展，分析了基于[4 + 2]两组分环缩合的经典方法的改进以及新颖的多组分方法，这些方法大多基于[3 + 2] +1]三成分策略，不仅具有合成效率，而且在环境相容性方面也非常具有吸引力。