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