Synthesis of 4-substituted 3, 3-difluoropiperidines

…, G Macdonald, F Deroose, N De Kimpe

文献索引：Surmont, Riccardo; Verniest, Guido; Thuring, Jan Willem; Macdonald, Gregor; Deroose, Frederik; De Kimpe, Norbert Journal of Organic Chemistry, 2010 , vol. 75, # 3 p. 929 - 932

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被引用次数: 21

摘要

Synthetic strategies toward 4-substituted 3, 3-difluoropiperidines were evaluated. 4- Alkoxymethyl-and 4-aryloxymethyl-3, 3-difluoropiperidines were synthesized via 1, 4- addition of ethyl bromodifluoroacetate to 3-substituted acrylonitriles in the presence of copper powder, followed by borane reduction of the cyano substituent, lactamization, and reduction of the lactam. This method was applied to establish the synthesis of N-protected ...