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Using thianthrene S-oxide (TTSO) as a transient mediator, para-arylation and alkenylation of mono-substituted arenes have been demonstrated via a para-selective thianthrenation/Pd-catalyzed thio-Suzuki-Miyaura coupling sequence under mild conditions. This reaction features a broad substrate scope, and functional group and heterocycle tolerance. The versatility of this approach was further demonstrated by late-stage functionalization of complex bioactive scaffolds, and direct synthesis of some pharmaceuticals, including Tetriprofen, Ibuprofen, Bifonazole, and LJ570.
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Reference:
Patent; SANOFI; US2011/294788; (2011); A1;,
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