A practical synthesis of 3,4-diethoxybenzthioamide based on Friedel-Crafts reaction with potassium thiocyanate in methanesulfonic acid.

Bioorg Med Chem Lett

Process Research Laboratory, 2nd Tokushima Factory, Otsuka Pharmaceutical Co., Ltd., 224-18, Ebisuno, Hiraishi, Kawauchi-cho, Tokushima 771-0182, Japan.

Published: September 2002

The synthesis of 3,4-diethoxybenzthioamide, the key intermediate for OPC-6535, is achieved by employing Friedel-Crafts reaction of 1,2-diethoxybenzene with potassium thiocyanate in methanesulfonic acid at ambient temperature.

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http://dx.doi.org/10.1016/s0960-894x(02)00398-0DOI Listing

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