Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Universidade de Vigo, 36310, Vigo, Spain.
Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Universidade de Vigo, 36310, Vigo, Spain.
Eur J Med Chem. 2019 Jan 1;161:468-478. doi: 10.1016/j.ejmech.2018.10.047. Epub 2018 Oct 25.
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.
酞嗪-1(2H)-酮是一种二氮杂并环戊二烯，存在于各种与化学的多个分支相关的合成分子中，包括药物化学。酞嗪酮核心在药物发现中的多功能性促进了对新的合成方法的探索，以获得不同取代和功能化的衍生物。本文综述了与药物发现过程相关的酞嗪酮衍生物合成的最新进展，分析了基于[4+2]二组分环缩合的经典方法的改进以及基于[3+2+1]三组分策略的新型多组分方法，这些方法不仅因为其合成效率，而且在环境相容性方面也非常有吸引力。
