A Convenient Synthesis of Novel 2,8-Disubstituted Pyrido[3,4-b]pyrazines Possessing Biological Activity

作者：Antoine Maud; Gerlach Matthias; Guenther Eckhard; Schuster Tilmann; Czech Michael; Seipelt Irene; Marchand Pascal^*

来源：Synthesis (Germany), 2012, 44(1): 69-82.

DOI：10.1055/s-0031-1289613

• pyrido[3,4-b]pyrazines
• pyridines
• thioacetals
• phenylglyoxals
• regioselectivity
• condensation

A regioselective synthetic route to 2,8-disubstituted pyrido[3,4-b]pyrazines, by initial condensation reaction between suitable diaminopyridines and alpha-keto aldehydes equivalents, has been developed. Focusing on the functionalization on C-8, 2-ary1-8-bromo- and 8-amino-2-arylpyrido[3,4-b]pyrazines have been synthesized. Anilines, amides, and ureas have been introduced at the 8-position from key intermediates. 2,8-Disubstituted pyrido[3,4-b]pyrazines thus prepared were found to be of biological interest.

• 出版日期2012-1-2