Ugi three-component coupling reaction for the synthesis of 2-(6-oxo-11-phenyl-7,8-dihydrobenzo[b]pyrrolo[1,2-d][1,4]diazocin-5(6H)-yl)-2-phenylacetamide derivatives

- It is a three-component, four center Ugi reaction.
- It is very useful to technique to construct eight-membered pyrrolo[1,2-d][1,4]diazacines.
- It involves a bifunctional amine tethered carboxylic acid based 3CC reaction.
- It provides an easy access to generate combinatorial libraries of pyrrolo[1,2-d][1,4]diazacines for drug discovery.

A three-component, four center Ugi reaction of 3-(1-(2-aminophenyl)-5-phenyl-1H-pyrrol-2-yl)propanoic acid with aromatic aldehyde and t-butyl isocyanide has been achieved to produce a novel class of N-tert-butyl-2-(6-oxo-11-phenyl-7,8-dihydrobenzo[b]pyrrolo[1,2-d][1,4]diazacine-5(6H)-yl)-2-phenylacetamides in moderate to good yields.