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A Novel Practical Synthesis of Benzothiazoles via Pd-Catalyzed Thiol Cross-Coupling

Takahiro Itoh* and Toshiaki Mase

*Merck Research Laboratories, Merck & Co., Inc., RY50G-132, 126 East Lincoln Avenue, P.O. Box 2000, Rahway NJ 07065-0900, Email:

T. Itoh, T. Mase, Org. Lett., 2007, 9, 3687-3689.

DOI: 10.1021/ol7015737


Various 2-bromoanilides were reacted with 2-ethylhexyl 3-mercaptopropionate in high yields using a palladium catalyst. Subsequent generation of thiols and condensation under basic or acidic conditions allows a convenient synthesis of substituted benzothiazoles.

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ID: J54-Y2007-2910