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Development of an Industrial Process Based on the Groebke-Blackburn-Bienaymé Multicomponent Reaction: Efficient Preparation of 3-Aminoimidazo[1,2-a]pyrazines

Markus Baenziger*, Estelle Durantie, Christian Mathes

*Novartis Pharma AG, Postfach, 4002 Basel, Switzerland, Email: markus.baenzigernovartis.com

M. Baenziger, E. Durantie, C. Mathes, Synthesis, 2017, 49, 2266-2274.

DOI: 10.1055/s-0036-1588130 (free Supporting Information)



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Abstract

The 3-Aminoimidazo[1,2-a]pyrazine scaffold is rapidly accessible through a Groebke-Blackburn-Bienaymé cyclisation starting from an aminopyrazine, an aldehyde and an isocyanide. A scale-up process of this multicomponent reaction has been achieved in high yield and with excellent purity.


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Key Words

cyclisation, fused N-heterocycles, Groebke-Blackburn-Bienaymé Reaction, one-pot process, sulfate salt


ID: J66-Y2017