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Efficient route to 6-CF3-substituted nicotinic acid derivatives
Authors:Valentine G. Nenajdenko  Sergey V. Druzhinin  Elizabeth S. Balenkova
Affiliation:Moscow State University, Department of Chemistry, Leninskie Gory, Moscow 119992, Russia
Abstract:A novel synthetic sequence for preparation of CF3-pyridines is presented. Reaction of α,β-unsaturated trifluoromethylketones with α-cyanoketones leads to α-hydroxydihydropyranes 1 containing CF3-group. α-Hydroxydihydropyranes can be easily transformed to α-hydroxytetrahydropyridines, 1,4-dihydropyridines and CF3-pyridines. All CF3-pyridine derivatives were obtained in good yields. This route can be applied for preparation of CF3-pyridines containing various substituents with further possible modification on cyano-group.
Keywords:α,β-Unsaturated trifluoromethylketones   α-Hydroxydihydropyranes   α-Hydroxytetrahydropyridines   1,4-Dihydropyridines   CF3-pyridines
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