Synthesis of N tau-arylhistidine derivatives via direct N-arylation.

Bioorg Med Chem Lett, 2004/4/05;14(7):1637-40.

Yue W[1], Lewis SI, Koen YM, Hanzlik RP

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PMID: 15026040

Impact factor: 2.94

Abstract
N(tau)-Aryl-histidine derivatives were synthesized using a modified one-step Cu-catalyzed coupling of aryl halides and N-acetylhistidine methyl ester. The latter is much less reactive than imidazole toward aryl halides. p-Chloroiodobenzene coupled with iodine displacement only, whereas m- and p-bromoiodobenzene both gave mixtures of bromo- and iodophenyl products.
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