Solution-Phase Parallel Synthesis of Hexahydro-1H-isoindolone Libraries
Parallel solution phase synthesis of a series of libraries involving the synthesis of hexahydro-1H-isoindolones was performed exploiting a novel "tactical combination" of Cu-catalyzed three-component coupling and Diels-Alder reactions. Three distinct libraries consisting of 24, 60, and 32 members were constructed. Additional sub-libraries of isoindolone scaffolds were prepared in a one-pot/two-step process and further diversified via Pd-catalyzed Suzuki cross-coupling reaction with boronic acids.
Source: Zhang, Lushington, Neuenswander, Hershberger, and Malinakova. J. Comb. Chem., 10 (2), 285-302, 2008. University Department of Chemistry, Center for Chemical Methodologies and Library Development.
a-Alkylation of SAMP-Hydrazones
Reactions can be carried out in round bottom or fritted vessels in a variety of sizes. Purification and cleanup are simple: fritted reaction vessels, combined with the unique built-in valve, allow reaction products to be passed through scavenging resins in seconds. The following SAMP reaction required strictly anhydrous conditions at -70 in the presence of corrosive reagents. The reactions were successuflly carried out using MiniBlock fitted with inert atmosphere manifolds. The investigators repeated this reaction sequence in solid phase using a novel SAMP resin, resulting comparable yields.
Source: Prof D. Enders, J. Koebbberling RWTH Aachen, Germany.