An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives

We report the chemical design and development of 3-aryl-substituted 7-alkoxy-4-methylcoumarins with enhanced fluorogenic properties. The 3-aryl substituents are installed via an optimized Suzuki–Miyaura cross-coupling (SMC) reaction between a 7-alkoxy-3-bromo-4-methylcoumarin and aryl boronic MIDA e...

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Main Authors: Alhaj Zen, Amer, Aylott, Jonathan W., Chan, Weng C.
Format: Article
Published: Elsevier 2014
Subjects:
Online Access:https://eprints.nottingham.ac.uk/37547/
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author Alhaj Zen, Amer
Aylott, Jonathan W.
Chan, Weng C.
author_facet Alhaj Zen, Amer
Aylott, Jonathan W.
Chan, Weng C.
author_sort Alhaj Zen, Amer
building Nottingham Research Data Repository
collection Online Access
description We report the chemical design and development of 3-aryl-substituted 7-alkoxy-4-methylcoumarins with enhanced fluorogenic properties. The 3-aryl substituents are installed via an optimized Suzuki–Miyaura cross-coupling (SMC) reaction between a 7-alkoxy-3-bromo-4-methylcoumarin and aryl boronic MIDA esters using Pd(OAc)2/XPhos in a catalytic system with K2CO3 in aqueous THF. Under these conditions, an exocyclic ester functionality is found to be unaffected. Subsequent saponification revealed a carboxylic acid functionality that is suitable for conjugation reactions. Evaluation of their fluorescence properties indicated that the installed 3-heteroaryl substituent, particularly benzofuran-2-yl, resulted in a significant red shift of both the excitation and emission wavelengths.
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spelling nottingham-375472020-05-04T16:52:49Z https://eprints.nottingham.ac.uk/37547/ An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives Alhaj Zen, Amer Aylott, Jonathan W. Chan, Weng C. We report the chemical design and development of 3-aryl-substituted 7-alkoxy-4-methylcoumarins with enhanced fluorogenic properties. The 3-aryl substituents are installed via an optimized Suzuki–Miyaura cross-coupling (SMC) reaction between a 7-alkoxy-3-bromo-4-methylcoumarin and aryl boronic MIDA esters using Pd(OAc)2/XPhos in a catalytic system with K2CO3 in aqueous THF. Under these conditions, an exocyclic ester functionality is found to be unaffected. Subsequent saponification revealed a carboxylic acid functionality that is suitable for conjugation reactions. Evaluation of their fluorescence properties indicated that the installed 3-heteroaryl substituent, particularly benzofuran-2-yl, resulted in a significant red shift of both the excitation and emission wavelengths. Elsevier 2014-10-01 Article PeerReviewed Alhaj Zen, Amer, Aylott, Jonathan W. and Chan, Weng C. (2014) An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives. Tetrahedron Letters, 55 (40). pp. 5521-5524. ISSN 0040-4039 Coumarin Suzuki cross-coupling Arylboronic MIDA ester Fluorescence http://www.sciencedirect.com/science/article/pii/S0040403914013926 doi:10.1016/j.tetlet.2014.08.058 doi:10.1016/j.tetlet.2014.08.058
spellingShingle Coumarin
Suzuki cross-coupling
Arylboronic MIDA ester
Fluorescence
Alhaj Zen, Amer
Aylott, Jonathan W.
Chan, Weng C.
An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives
title An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives
title_full An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives
title_fullStr An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives
title_full_unstemmed An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives
title_short An appraisal of the Suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives
title_sort appraisal of the suzuki cross-coupling reaction for the synthesis of novel fluorescent coumarin derivatives
topic Coumarin
Suzuki cross-coupling
Arylboronic MIDA ester
Fluorescence
url https://eprints.nottingham.ac.uk/37547/
https://eprints.nottingham.ac.uk/37547/
https://eprints.nottingham.ac.uk/37547/