An Efficient, Regioselective Amination of 3,5-Disubstituted Pyridine N-Oxides Using Saccharin as an Ammonium Surrogate

作者：Farrell Robert P^*; Elipe Maria Victoria Silva; Bartberger Michael D; Tedrow Jason S; Vounatsos Filisaty

来源：Organic Letters, 2013, 15(1): 168-171.

DOI：10.1021/ol303218p

A process for the regioselective amination of unsymmetrical 3,5-substituted pyridine N-oxides has been developed utilizing cheap, readily available saccharin as an ammonium surrogate. High conversions of the corresponding saccharin adducts have been achieved under mild reaction conditions. In situ deprotection under acidic conditions allows for a one-pot process to substituted aminopyridines. High regioselectivities were obtained from a variety of 3,5-disubstituted pyridine N-oxides.

• 出版日期2013-1-4