Access to novel imidazo[1,5-a]pyrazine scaffolds by the combined use of a three-component reaction and a base-assisted intramolecular cyclization

作者：Attanasi Orazio A; Favi Gianfranco^*; Giorgi Gianluca; Majer Roberta; Perrulli Francesca Romana; Santeusanio Stefania

来源：Organic and Biomolecular Chemistry, 2014, 12(26): 4610-4619.

DOI：10.1039/c4ob00676c

A novel and practical two-step approach to an intriguing class of imidazo[1,5-a]pyrazines with exocyclic C=X (X = CH2, O) bonds is described. The process utilizes a sequential three-component reaction of propargyl amine or aminoester, 1,2-diaza-1,3-dienes and isothiocyanates to furnish functionalized 2-thiohydantoins which are transformed into thiohydantoin-fused tetrahydropyrazines by subsequent regioselective base-promoted cyclization.

• 出版日期2014