| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5269858 | Tetrahedron Letters | 2014 | 4 Pages |
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.
Graphical abstractThis Letter reports the first 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 oxidative workup. These acid intermediates were performed on gram scale and are perfect partners for library synthesis and have good physical and chemical properties for drug discovery.Download full-size image
