Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 161, Issue -, Pages 468-478Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.10.047
Keywords
Phthalazinone derivatives; Synthesis; Biological versatility; Cyclocondensations; Multicomponent reactions
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Funding
- Xunta de Galicia
- University of Vigo
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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 + 21 two-component cyclocondensations as well as novel multi component 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. (C) 2018 Elsevier Masson SAS. All rights reserved.
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