ChemInform Abstract: A Novel Base‐Mediated Intramolecular Hydroamination to Build Fused Heteroaryl Pyrazinones.

Abstract

Pyrazine derivatives R 0550A Novel Base-Mediated Intramolecular Hydroamination to Build Fused Heteroaryl Pyrazinones. -The procedure for the synthesis of title compounds (II), (IV) and (VI) is based on the DBU-mediated cyclization of amides of type (I), (III), and (V) where mixtures of double bond isomers (endo/exo-E, exo-Z) are formed. Their treatment according to B) renders possible the isolation of the thermodynamically most stabe isomer with concomitant loss of the -Dmb protecting group. -(LLAUGER*, L.; BERGAMI, C.; KINZEL, O. D.; LILLINI, S.; PESCATORE, G.; TORRISI, C.; JONES, P.; Tetrahedron Lett. 50 (2009) 2, 172-177; Dep. Med. Chem., Ist. Ric. Biol. Mol., I-00040 Pomezia, Italy; Eng.) -Mais 15-172