• From left: Dr. E. Durantie, Dr. M. Baenziger (top), Dr. C. Mathes (bottom) (Novartis Pharma, Basel, Switzerland)

    From left: Dr. E. Durantie, Dr. M. Baenziger (top), Dr. C. Mathes (bottom) (Novartis Pharma, Basel, Switzerland)

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Preparation of 3-Aminoimidazo[1,2-a]pyrazines

Estelle Durantie presents an industrial process to access 3-aminoimidazo[1,2-a]pyrazines.

Development of an Industrial Process Based on the Groebke–Blackburn–Bienaymé Multicomponent Reaction: Efficient Preparation of 3-Aminoimidazo[1,2-a]pyrazines: M. Baenziger, E. Durantie, C. Mathes
Synthesis 2017, 49, DOI: 10.1055/s-0036-1588130

3-Aminoimidazo[1,2-a]pyrazines are important building blocks for the pharmaceutical and agrochemical industries, as this structural motif is present in a variety of drug candidates and constitutes a valuable sub-structure in combinatorial libraries. The scale-up of the synthesis of 3-aminoimidazo[1,2-a]pyrazines can be a key step in drug development. Recently, the group of Dr. Estelle Durantie at Novartis Pharma (Basel, Switzerland) has reported an important research work aimed at facilitating an industrial-scale preparation of the title compounds.

  • One-pot, two-step procedure to synthesize 3-aminoimidazo[1,2-a]pyrazines

    One-pot, two-step procedure to synthesize 3-aminoimidazo[1,2-a]pyrazines

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Dr. Durantie said:

“Multicomponent reactions can be challenging when it comes to scaling-up. By developing a one-pot, two-step process, the Groebke–Blackburn–Bienaymé cyclization can easily and efficiently access 3-aminoimidazo[1,2-a]pyrazines which are important motifs in biologically active molecules.” 

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