Abstract
A base-promoted strategic synthesis of various functionalized thiomethylated-benzenes has been established from aryl/heteroaryl/cyclopropyl methyl ketone. We can directly access the thiomethylated-benzene nucleus embedded with diverse functional group by the reaction of 3,3-bis(methylthio)-1-arylprop-2-en-1-ones and 2-(1-aryl/cyclopropyl)ethylidene)malononitriles in the presence of sodium hydride in THF at reflux temperature. These precursors are easily accessible from aryl methyl ketones. Various functional groups like alkyl, aryl, nitrile, amine, aroyl and thiomethyl can be directly installed to the benzene ring. The one-pot approach for the construction of thiomethylated-benzene nucleus was also developed. The structure of the synthesized compound was confirmed by X-ray crystallography.
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