Silver mediated direct C–H arylation of 3-bromoisothiazole-5-carbonitrile
作者： Andreas S. Kalogirou , Panayiotis A. Koutentis
DOI: 10.1016/J.TET.2014.07.064
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摘要: Abstract Palladium catalyzed direct C–H arylation of 3-bromoisothiazole-5-carbonitrile with aryl/hetaryl iodides in the presence AgF gave 13 4-aryl/hetaryl-3-bromoisothiazole-5-carbonitriles. The scope this was investigated and explanations for limitations proposed. 3-Bromoisothiazole-5-carboxamide isolated as a side-product, its formation attributed to Ag+-catalyzed hydration C-5 nitrile. analogous phenylation 3-chloroisothiazole-5-carbonitrile 3-bromoisothiazole-4-carboxamide 3-chloro-4-phenylisothiazole-5-carbonitrile 3-bromo-5-phenylisothiazole-4-carboxamide 83 64% yields, respectively.
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