Recent advances in the synthesis of phthalazin-1(2H)-one core as a relevant pharmacophore in medicinal chemistry.


Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
01 Jan 2019
Historique:
received: 17 07 2018
revised: 18 10 2018
accepted: 19 10 2018
pubmed: 6 11 2018
medline: 19 12 2018
entrez: 3 11 2018
Statut: ppublish

Résumé

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.

Identifiants

pubmed: 30388463
pii: S0223-5234(18)30916-4
doi: 10.1016/j.ejmech.2018.10.047
pii:
doi:

Substances chimiques

Phthalazines 0

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

468-478

Informations de copyright

Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Auteurs

Carmen Terán (C)

Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Universidade de Vigo, 36310, Vigo, Spain. Electronic address: mcteran@uvigo.es.

Pedro Besada (P)

Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Universidade de Vigo, 36310, Vigo, Spain.

Noemí Vila (N)

Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Universidade de Vigo, 36310, Vigo, Spain.

Ma Carmen Costas-Lago (MC)

Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Universidade de Vigo, 36310, Vigo, Spain.

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Classifications MeSH