Synthesis of 5-alkyl-4-amino-2-(trifluoromethyl)pyridines and their transformation into trifluoromethylated 1H-pyrazolo[4,3-c]pyridines

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• 作者：Tyvorskii ; Vladimir I. ; Bobrov ; Denis N. ; Kulinkovich ; Oleg G. ; Tehrani ; Kourosch Abbaspour ; et. al.
• 关键词：4H-pyran-4-ones ; 4-aminopyridines ; 1H-pyrazolo[4 ; 3-c]pyridines ; Smiles rearrangement
• 刊名：Tetrahedron
• 出版年：2001
• 出版时间：March 3, 2001
• 年：2001
• 卷：57
• 期：10
• 页码：2051-2055
• 全文大小：111 K

文摘

5-Alkyl-4-amino-2-(trifluoromethyl)pyridines were prepared in good yields starting from the corresponding pyridinols either using condensation with tosyl isocyanate or by alkylation with 2-chloroacetamide and subsequent Smiles type rearrangement. The cyclisation of diazonium salts, generated from 5-alkyl-4-amino-2-(trifluoromethyl)pyridines, afforded trifluoromethylated 1H-pyrazolo[4,3-c]pyridines.