Traceless Solid Phase Synthesis of Bicyclic Dihydropyrimidone Libraries Using Microwave-Assisted Cyclization Cleavage
Poster Jul 25, 2006
Rolando Pérez, Doris Dallinger and C. Oliver Kappe
4-Aryl-3,4-dihydro-2(1H)-pyrimidone esters ("Biginelli compounds", DHPMs) represent a heterocyclic system of remarkable pharmacological efficiency. More recently, appropriately functionalized DHPMs have emerged as potent calcium channel blockers, antihypertensive agents, a1a -adrenergic antagonists, mitotic kinesin Eg5 inhibitors and neuropeptide Y (NPY) antagonists. In recent years several different pathways for the synthesis of DHPMs have been reported, including combinatorial approaches, using e.g. solid phase reaction conditions. We now report a variation of the Biginelli condensation using methyl 4-chloroacetoacetate as the building block both in solution and in solid phase. This modification allows the rapid entry into a variety of bicyclic heterocyclic ring scaffolds.
CiPA Phase 2 Study: validation of an automated microelectrode array (MEA) assay of hiPSC-derived cardiomyocyte electrophysiology for cardiac safety evaluationPoster
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
A luminescent solar concentrator-based photomicroreactor for energy efficient continuous-flow photocatalysisPoster
The Luminescent Solar ConcentratorPhotomicroreactor
(LSC-PM) is an innovative device
for solar-powered continuous-flow photochemistry.