Efficient Halogenation of 2-Aminopyrazine

Dolors Pujol presents an efficient method for the halogenation of 2-aminopyrazine.

Efficient Halogenation of 2-Aminopyrazine: E. Lizano, J. Grima, M. D. Pujol
Synlett 2019, DOI: 10.1055/s-0039-1690183

Halogenated 2-aminopyrazines are very useful functionalized starting products for the synthesis of nitrogen heterocycles, which include drugs and bioactive compounds. Recently, the group of Professor Maria Dolors Pujol from the University of Barcelona (Spain) reported a detailed study on the halogenation of 2-aminopyrazine.



Professor Pujol said: “We have developed a method and set up conditions that allow preparation of both 2-amino-5-bromopyrazine and 2-amino-3,5-dibromopyrazine in excellent yields depending on the amount of halogenating agent added. Acetonitrile has proven to be the ideal solvent and the assistance of microwave irradiation is essential to obtain halogenated 2-aminopyrazine.” 

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