A novel practical synthesis of benzothiazoles via Pd-catalyzed thiol cross-coupling |
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Authors: | Itoh Takahiro Mase Toshiaki |
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Institution: | Process Research, PreClinical Development, Banyu Pharmaceutical Co., Ltd., 3 Okubo, Tsukuba, Ibaraki, 300-2611, Japan. takahiro_itoh@merck.com |
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Abstract: | A convenient synthesis of substituted benzothiazoles from 2-bromoanilides has been accomplished. The various 2-bromoanilides were reacted with an alkyl thiolate in high yields using a palladium catalyst. The resulting sulfides were easily converted to the corresponding benzothiazoles via the simultaneous generation of thiols and condensation under basic or acidic conditions. |
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