an efficient synthesis of 1,4-dihydro-6-trifluoromethylpyridines: a facile and useful method for...

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2007 Pyridine derivatives R 0380 An Efficient Synthesis of 1,4-Dihydro-6-trifluoromethylpyridines: A Facile and Useful Method for Dehydration of α-Trifluoromethyl Alcohols by Use of Phospho- rus Oxychloride/Pyridine Adsorbed on Silica Gel. — Reaction of unsaturated ke- tones (I) with β-aminocrotonates (II) affords 2-hydroxy-2-trifluoromethyltetrahydro- pyridines, which are dehydrated in situ by use of phosphorus oxychloride/pyridine ad- sorbed on silica gel. Reactive functional groups such as esters are stable under the re- action conditions. — (KATSUYAMA*, I.; FUNABIKI, K.; MATSUI, M.; MURAMATSU, H.; SHIBATA, K.; Heterocycles 68 (2006) 10, 2087-2096; Hitec Co., Ltd., Kitaku, Osaka 530, Japan; Eng.) — R. Langenstrassen 07- 117

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Page 1: An Efficient Synthesis of 1,4-Dihydro-6-trifluoromethylpyridines: A Facile and Useful Method for Dehydration of α-Trifluoromethyl Alcohols by Use of Phosphorus Oxychloride/Pyridine

2007

Pyridine derivativesR 0380 An Efficient Synthesis of 1,4-Dihydro-6-trifluoromethylpyridines: A Facile and

Useful Method for Dehydration of α-Trifluoromethyl Alcohols by Use of Phospho-rus Oxychloride/Pyridine Adsorbed on Silica Gel. — Reaction of unsaturated ke-tones (I) with β-aminocrotonates (II) affords 2-hydroxy-2-trifluoromethyltetrahydro-pyridines, which are dehydrated in situ by use of phosphorus oxychloride/pyridine ad-sorbed on silica gel. Reactive functional groups such as esters are stable under the re-action conditions. — (KATSUYAMA*, I.; FUNABIKI, K.; MATSUI, M.; MURAMATSU, H.; SHIBATA, K.; Heterocycles 68 (2006) 10, 2087-2096; Hitec Co., Ltd., Kitaku, Osaka 530, Japan; Eng.) — R. Langenstrassen

07- 117