Chloroamine serves as an efficient amination reagent to the heteroaromatic C-H bond of azole under copper catalysis even at room temperature. This catalysis enables a rapid and concise construction of aminoazoles of great interest in biological and medicinal chemistry.
Efficient Phosphonium-Mediated Synthesis of 2-Amino-1,3,4-oxadiazoles
作者:Christopher G. Levins、Zhao-Kui Wan
DOI:10.1021/ol8004084
日期:2008.5.1
We present an efficient, room temperature procedure for the preparation of 2-amino-1,3,4-oxadiazoles, Oxadiazol-2-ones can be activated for S(N)Ar substitution using phosphonium reagents (e.g., BOP). This approach provides convenient access to N,N-disubstituted 2-amino-1,3,4-oxadiazoles, which are difficult to prepare using existing synthetic strategies.
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