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Expedient Drug Synthesis and Diversification via ortho-C−H Iodination using Recyclable PdI2 as the Precatalyst

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journal contribution
posted on 16.07.2010, 00:00 by Tian-Sheng Mei, Dong-Hui Wang, Jin-Quan Yu
Pd(II)-catalyzed ortho-C−H iodination reactions of phenylacetic acid substrates have been achieved using recyclable PdI2 as the precatalyst. This class of substrates is incompatible with the classic amide formation/ortho-lithiation/iodination sequence. The power of this new technology is demonstrated by facile drug functionalization and drastically shortened syntheses of the drugs diclofenac and lumiracoxib.

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