Iodine-promoted facile synthesis of new (+)-2,3-dihydro-N,2-diarylquinazolines
摘要:
The reactivity of 2-amino-N'-arylbenzamidines 1a-e towards p-tolualdehyde 2a and 1-naphthaldehyde 2b under the catalytic influence of commercial iodine at ambient temperature has been examined. New chiral quinazolines 3a-e and 4a-d have been identified as reaction products. These products have subsequently been oxidised to N,2-diarylquinazolin-4-amines 12, 13a-d. The structures of the products were elucidated by their NMR, mass and IR spectra in addition to elemental analyses. The structure of 3e was further confirmed by X-ray structural analysis. The mechanism of formation of 3a-e and 4a-d is discussed.
The Suzuki-Miyaura coupling between 2-chloro-4-aminoquinazolines and arylboronic acids catalyzed by the well-defined N-heterocyclic carbene-PdCl2-1-methylimidazole complex was performed at room temperature, giving the desired products in good to high yields. Through this methodology, a variety of 2-aryl-4-aminoquinazoline derivatives with potential pharmaceutical activities can be achieved under mild reaction conditions. (C) 2020 Elsevier Ltd. All rights reserved.
[EN] METHODS AND MATERIALS FOR INCREASING TRANSCRIPTION FACTOR EB POLYPEPTIDE LEVELS<br/>[FR] PROCÉDÉS ET MATÉRIAUX POUR AUGMENTER LES NIVEAUX DE POLYPEPTIDES EB DE FACTEUR DE TRANSCRIPTION
This document provides methods and materials for increasing TFEB polypeptide levels. For example, compounds (e.g., organic compounds) having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, formulations containing compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for making compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for making formulations containing compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for increasing TFEB polypeptide levels within cells and/or within a nucleus of cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in TFEB polypeptide levels are provided.
Iodine-promoted facile synthesis of new (+)-2,3-dihydro-N,2-diarylquinazolines
作者:Kamal M. El-Shaieb、Henning Hopf、Peter G. Jones
DOI:10.3998/ark.5550190.0011.a09
日期:——
The reactivity of 2-amino-N'-arylbenzamidines 1a-e towards p-tolualdehyde 2a and 1-naphthaldehyde 2b under the catalytic influence of commercial iodine at ambient temperature has been examined. New chiral quinazolines 3a-e and 4a-d have been identified as reaction products. These products have subsequently been oxidised to N,2-diarylquinazolin-4-amines 12, 13a-d. The structures of the products were elucidated by their NMR, mass and IR spectra in addition to elemental analyses. The structure of 3e was further confirmed by X-ray structural analysis. The mechanism of formation of 3a-e and 4a-d is discussed.