An efficient protocol for the preparation of 4,5-functionalised 2-amino-1H-imidazoles
as fragment-like structures was developed in isolated yields up to 95 %. The demonstrated
one-pot manner includes an intramolecular oxidative annulation and ring cleavage sequence
starting from Mannich precursors. The suggested one-pot sequential synthetic methodology
is easy to apply in automatic and robotic chemistry laboratories for which a rapidly
increasing demand is foreseen because of the ongoing revolution in the field of continuous
manufacturing of pharmaceutical drug substances and products. Further transformation
utilities such as Groebke-Blackburn-Bienayme 3CR and the formation of marine alkaloid
analogs were also represented.
