1-Bromo-2-trifluoroacetylcyclobutenes as novel building blocks for the construction of trifluoromethyl substituted heterocycles. Part 2: Synthesis of trifluoromethyl substituted thiophenes, condensed with cyclobutene moieties
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AbstractThis paper describes a novel synthetic approach to 2-cyano-3-trifluoromethylthiophenes fused with cyclobutene rings with variable spiro conjunctions. The reaction of substituted 1-bromo-2-trifluoroacetylcyclobutenes with mercaptoacetonitrile results in the substitution of bromine with S-center to afford the corresponding nitriles in high yields, which form the target thiophenes by subsequent treatment of lithium 2,2,6,6-tetramethylpiperidide and acetic anhydride.

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