期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 7, 期 20, 页码 4271-4278出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/b912033e
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- CNRS
An efficient site selective method for the direct arylation of free-(NH2) adenines 1 to provide a range of C-8 arylated adenines 3 in excellent yields is described. This process based on the use of Pd(OH)(2)/C as the catalyst and a stoichiometric amount of CuI under ligandless conditions is general. It allows the coupling to proceed with a variety of aryl halides, including for the first time cheaper and less reactive aryl chlorides. The extension of this process for the sequential preparation of non-symmetrical C8/N-6-arylated adenines 4 is also reported.
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