PROCESS FOR PRODUCING 2-SUBSTITUTED BENZO[b]THIOPHENE

摘要

An industrial process for producing a 2-substituted benzo[b]thiophene which is highly effective in that it can afford the target compound in a high yield with a simple operation without the necessity for using unstable starting materials. The process comprises reacting an optionally substituted 2-halogenobenzaldehyde with either a compound represented by the general formula (1): HiSjMk (wherein M represents an alkali metal atom; i represents an integer of 0 or 1; j represents an integer of 1 or above; and k represents an integer of 1 or 2; provided i + k = 2) and sulfur, or a compound represented by the above formula (1) (wherein j is 2 or above) in the presence of an aprotic polar solvent, and then reacting the reaction product with a compound represented by the general formula (2): XCH2R (wherein X represents a halogen atom; and R represents acyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, or cyano) to effect intramolecular ring closure.