Direct synthesis of N-aryl/alkyl 3-carbonylpyrroles from the Morita-Baylis-Hillman acetate of 2,2-dimethoxyacetaldehyde and a primary amine

N-Aryl/alkyl 3-carbonylpyrroles are ubiquitous in compounds of biological and material significance, whereas their synthesis traditionally requires a multistep protocol. Herein a kalinite catalyzed direct synthesis of N-substituted 3-carbonylpyrroles from a 2,2-dimethoxyacetaldehyde derived Morita-Baylis-Hillman acetate and a primary amine in ethanol is developed. This reaction is scalable and also applicable to the synthesis of JMH-030, JMC-2004 and other bioactive compounds.

Automated summary

A direct synthesis method catalyzed by kalinite has been developed for the efficient preparation of N-substituted 3-carbonylpyrroles, with potential applications in biological and material fields.