A novel and effective approach to 4-fluoropyrimidines

作者：Sedenkova Kseniya N; Averina Elena B^*; Grishin Yuri K; Kuznetsova Tamara S; Zefirov Nikolay S

来源：Tetrahedron Letters, 2014, 55(2): 483-485.

DOI：10.1016/j.tetlet.2013.11.070

• 4-Fluoropyrimidine N-oxides
• 4-Fluoropyrimidines
• Reduction
• Aromatic nucleophilic substitution

A series of 4-fluoropyrimidine 1-oxides, obtained via three-component heterocyclization, was studied under various reduction conditions. An effective preparative method for the synthesis of 4-fluoropyrimidines from readily available starting materials was elaborated. 4-Fluoro-substituted tetrahydroquinazolines and tetrahydroquinazoline N-oxides were demonstrated to be highly reactive in aromatic nucleophilic substitution.

• 出版日期2014-1-8