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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

Baenziger, Markus and Durantie, Estelle and Mathes, Christian (2017) Development of an Industrial Process Based on the Groebke– Blackburn–Bienaymé Multicomponent Reaction: Efficient Preparation of 3-Aminoimidazo[1,2-a]pyrazines. Synthesis.

Abstract

Abstract 3-aminoimidazo[1,2,a]pyrazine is an important scaffold found in many drugs. This scaffold is rapidly accessible via a Groebke–Blackburn-Bienaymé cyclisation starting from an aminopyrazine, an aldehyde and an isocyanide. A scale-up process of this multicomponent reaction has been successfully achieved in high yield and excellent purity. The scope and limitations of this process leading to various 3 aminoimidazo[1,2,a]pyrazines are disclosed.

Item Type: Article
Keywords: 3 aminoimidazo[1,2,a]pyrazines, Groebke-Blackburn-Bienaymé reaction; one-pot process; multicomponent reaction.
Date Deposited: 04 Feb 2017 00:45
Last Modified: 04 Feb 2017 00:45
URI: https://oak.novartis.com/id/eprint/30759

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