Rapid Scaffold Decoration of Dihydropyrimidine Derivatives by Microwave-Assisted Solution Phase Synthesis
Introduction
The heterocyclic pyrimidine derivatives 1 (DHPMs) derived from the acid-catalyzed condensation of a b-ketoester, aldehyde and (thio)urea building block (Biginelli condensation) represents a “privileged scaffold” with remarkable pharmacological properties.1 In recent work we have reported the generation of a diverse library of DHPMs, employing an automated, sequential microwave-assisted solution phase strategy.2 We now present the high-speed microwave scaffold decoration around the DHPM heterocyclic core exploiting the diversity on at least six positions.
The heterocyclic pyrimidine derivatives 1 (DHPMs) derived from the acid-catalyzed condensation of a b-ketoester, aldehyde and (thio)urea building block (Biginelli condensation) represents a “privileged scaffold” with remarkable pharmacological properties.1 In recent work we have reported the generation of a diverse library of DHPMs, employing an automated, sequential microwave-assisted solution phase strategy.2 We now present the high-speed microwave scaffold decoration around the DHPM heterocyclic core exploiting the diversity on at least six positions.
