Selective arylation of phenol protected propygyl bromide via pd-catalysed Suzuki coupling reaction: synthesis, mechanistic studies by DFT calculations and their pharmacological aspects
Biaryls are the potential source of synthetic drugs. The present study describes the synthesis of a series of functionalized biphenyl derivatives (3a-3g) using Pd-catalyzed Suzuki coupling reaction. The experimental results revealed the facile synthesis of biphenyl derivatives (3a-3g) with notably h...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Polish Pharmaceutical Society
2018
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| Subjects: | |
| Online Access: | http://umpir.ump.edu.my/id/eprint/23928/ http://umpir.ump.edu.my/id/eprint/23928/ http://umpir.ump.edu.my/id/eprint/23928/ http://umpir.ump.edu.my/id/eprint/23928/1/Selective%20arylation%20of%20phenol%20protecteddone.pdf |
| Summary: | Biaryls are the potential source of synthetic drugs. The present study describes the synthesis of a series of functionalized biphenyl derivatives (3a-3g) using Pd-catalyzed Suzuki coupling reaction. The experimental results revealed the facile synthesis of biphenyl derivatives (3a-3g) with notably high yield (80-88%). Density functional theory (DFT) studies were performed by Gaussian 09 software in order to rationalize the
selectivity of coupling at C-Br bond instead of C-Cl bond. In addition of synthesis, the biological activities (biofilm inhibition, hemolytic and anti-thrombolytic) of these novel compounds were investigated. These results exhibited good biofilm inhibition (5.86-65.8%), hemolytic (1.32-30.1%) and anti-thrombolytic activities (9.64-42.5%), indicating the potential use of these compounds for pharmaceutical applications |
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