Scaffold Decoration at the N3-Position of Dihydropyrimidine Derivatives by Microwave-Assisted Solution Phase Synthesis
Poster May 14, 2006
Doris Dallinger and C. Oliver Kappe
In the library synthesis of N3-acylated DHPMs, different scavenging techniques using polymer-supported sequestration agents are described for the purification steps. In both synthesis and purification microwave flash heating was utilized, reducing reaction times from hours to minutes. In order to introduce novel diversity in the N3-position of the DHPM-scaffold, N3-arylations were performed by applying classical Cu (I)-catalyzed Goldberg reaction conditions under microwave heating.
These results support the use of hSC-CM and MEA technology for preclinical assessment of proarrhythmic risk within the proposed CiPA paradigm, and, more generally, demonstrate that automation of the CM-MEA assay can achieve high reliability and throughput for cardiac risk assessment in vitro.READ MORE