A Practical Synthesis of 3,4-Diethoxybenzthioamide Based on Friedel–Crafts Reaction with Potassium Thiocyanate in Methanesulfonic Acid

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. The synthesis of 3,4-diethoxybenzthioamide is reported.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-09, Vol.12 (17), p.2317-2320
Hauptverfasser:	Aki, Shinji, Fujioka, Takafumi, Ishigami, Masashi, Minamikawa, Jun-ichi
Format:	Artikel
Sprache:	eng
Schlagworte:	Chemistry Exact sciences and technology Indicators and Reagents Mesylates Noncondensed benzenic compounds Organic chemistry Preparations and properties Superoxides - antagonists & inhibitors Thiazoles - chemical synthesis Thioamides - chemical synthesis Thiocyanates
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Beschreibung
Zusammenfassung:	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. The synthesis of 3,4-diethoxybenzthioamide is reported.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00398-0