通过使用可回收的 PdI2 作为前催化剂进行邻位 C-H 碘化实现方便的药物合成和多样化。
Expedient drug synthesis and diversification via ortho-C-H iodination using recyclable PdI2 as the precatalyst.
机构信息
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
出版信息
Org Lett. 2010 Jul 16;12(14):3140-3. doi: 10.1021/ol1010483.
PMID:20550215
Abstract
Pd(II)-catalyzed ortho-C-H iodination reactions of phenylacetic acid substrates have been achieved using recyclable PdI(2) 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.
摘要
Pd(II)催化的苯乙酸底物的邻位 C-H 碘化反应已经实现，使用可回收的 PdI(2)作为前催化剂。这类底物与经典的酰胺形成/邻位锂化/碘化序列不兼容。该新技术的强大之处在于可以轻松地对药物进行功能化，并大大缩短了双氯芬酸和鲁米昔布等药物的合成。
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