An environmentally-friendly one-pot synthesis of 4-sulfonyl benzoic acids
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Add time:08/22/2019 Source:sciencedirect.com
This Letter reports an environmentally-friendly one-pot SNAr reaction of thiols to 4-halobenzoic acid methyl esters to provide 4-substituted sulfone benzoic acids and picolinic acids after bleach-mediated oxidative workup. These acid intermediates were synthesized on gram scale, are perfect partners for library synthesis, and have good physical chemical properties useful for drug discovery.
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