Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs

Diversity-Oriented Synthesis (DOS) represents a strategy to obtain molecule libraries with diverse structural features starting from one common compound in limited steps of synthesis. During the last two decades, DOS has become an unmissable strategy in organic synthesis and is fully integrated in v...

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Autores principales: Mathias Eymery, Viet-Khoa Tran-Nguyen, Ahcène Boumendjel
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Lenguaje:EN
Publicado: MDPI AG 2021
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Acceso en línea:https://doaj.org/article/dc39d14d38f4488890e2fd62eeb64766
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spelling oai:doaj.org-article:dc39d14d38f4488890e2fd62eeb647662021-11-25T18:39:33ZDiversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs10.3390/ph141111271424-8247https://doaj.org/article/dc39d14d38f4488890e2fd62eeb647662021-11-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1127https://doaj.org/toc/1424-8247Diversity-Oriented Synthesis (DOS) represents a strategy to obtain molecule libraries with diverse structural features starting from one common compound in limited steps of synthesis. During the last two decades, DOS has become an unmissable strategy in organic synthesis and is fully integrated in various drug discovery processes. On the other hand, natural products with multiple relevant pharmacological properties have been extensively investigated as scaffolds for ligand-based drug design. In this article, we report the amino dimethoxyacetophenones that can be easily synthesized and scaled up from the commercially available 3,5-dimethoxyaniline as valuable starting blocks for the DOS of natural product analogs. More focus is placed on the synthesis of analogs of flavones, coumarins, azocanes, chalcones, and aurones, which are frequently studied as lead compounds in drug discovery.Mathias EymeryViet-Khoa Tran-NguyenAhcène BoumendjelMDPI AGarticleDiversity-Oriented Synthesisnatural productsamino acetophenonesflavonesauronescoumarinsMedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1127, p 1127 (2021)
institution DOAJ
collection DOAJ
language EN
topic Diversity-Oriented Synthesis
natural products
amino acetophenones
flavones
aurones
coumarins
Medicine
R
Pharmacy and materia medica
RS1-441
spellingShingle Diversity-Oriented Synthesis
natural products
amino acetophenones
flavones
aurones
coumarins
Medicine
R
Pharmacy and materia medica
RS1-441
Mathias Eymery
Viet-Khoa Tran-Nguyen
Ahcène Boumendjel
Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs
description Diversity-Oriented Synthesis (DOS) represents a strategy to obtain molecule libraries with diverse structural features starting from one common compound in limited steps of synthesis. During the last two decades, DOS has become an unmissable strategy in organic synthesis and is fully integrated in various drug discovery processes. On the other hand, natural products with multiple relevant pharmacological properties have been extensively investigated as scaffolds for ligand-based drug design. In this article, we report the amino dimethoxyacetophenones that can be easily synthesized and scaled up from the commercially available 3,5-dimethoxyaniline as valuable starting blocks for the DOS of natural product analogs. More focus is placed on the synthesis of analogs of flavones, coumarins, azocanes, chalcones, and aurones, which are frequently studied as lead compounds in drug discovery.
format article
author Mathias Eymery
Viet-Khoa Tran-Nguyen
Ahcène Boumendjel
author_facet Mathias Eymery
Viet-Khoa Tran-Nguyen
Ahcène Boumendjel
author_sort Mathias Eymery
title Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs
title_short Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs
title_full Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs
title_fullStr Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs
title_full_unstemmed Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs
title_sort diversity-oriented synthesis: amino acetophenones as building blocks for the synthesis of natural product analogs
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/dc39d14d38f4488890e2fd62eeb64766
work_keys_str_mv AT mathiaseymery diversityorientedsynthesisaminoacetophenonesasbuildingblocksforthesynthesisofnaturalproductanalogs
AT vietkhoatrannguyen diversityorientedsynthesisaminoacetophenonesasbuildingblocksforthesynthesisofnaturalproductanalogs
AT ahceneboumendjel diversityorientedsynthesisaminoacetophenonesasbuildingblocksforthesynthesisofnaturalproductanalogs
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