Expeditious synthesis of chiral 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazines

Abstract

An expeditious one-pot two-step synthesis of chiral 4-substituted-6-methyl-1,2-dihydropyrrolo[1,2-a]pyrazin-3(4H)-ones via reaction between 5-methyl furfurylamine and N-Boc amino acids is described. LiAlH4-mediated reduction of 4-substituted-6-methyl-1,2-dihydropyrrolo[1,2-a]pyrazin-3(4H)-ones affords respective chiral 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazines in excellent yields.