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Synthesis of Thiophene-Based TAK-779 Analogues by C–H Arylation

Anna Junker, Junichiro Yamaguchi, Kenichiro Itami, and Bernhard Wünsch

J. Org. Chem. 2013, , Accepted Manuscript. DOI: 10.1021/jo400692p

Late-Stage Diversification Strategy

A rapid synthesis of thiophene-based TAK-779 analogues is reported using a late-stage diversification strategy. At the end of the synthesis, the key building block, which was prepared in six steps from thiophene, was arylated regioselectively at the α-position directly with iodoarenes.

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