Three-Component Synthesis of 2-Heteroaryl-3-hydroxybenzo[b]-thiophenes under Transition-Metal-Free Conditions

摘要

Main observation and conclusion A convenient synthetic route to 2-heteroaryl-3-hydroxybenzo[b]thiophene derivatives via K2CO3-promoted multicomponent cyclization between o-halogenated benzaldehyde, 2-methylquinolines and sulfur powder has been demonstrated. This reaction is performed smoothly under simple conditions to give the corresponding products in moderate to good yields. The resultant 3-hydroxybenzo[b]thiophenes have been proved to be versatile building blocks in a range of transition-metal-catalyzed cross-coupling reactions.

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