Solution-Phase Parallel Synthesis of a Library of ¢2-Pyrazolines

Manyem, S.; Sibi, M.; Lushington, G.; Neuenswander, B.; Schoenen, F.; Aube, J. Solution-Phase Parallel Synthesis of a Library of ¢2-Pyrazolines. J. Comb. Chem. 2007, 9, 20-28.

A parallel synthesis of a library (80 members) of 2-pyrazolines in solution phase is described. The 2-pyrazoline core was accessed through the [3 + 2] cycloaddition of nitrilimines with enoyl oxazolidinones. The cycloaddition provided two regioisomers, the major product being the C regioisomer. The oxazolidinone moiety was further reduced to the primary alcohol, producing another library of 5-hydroxymethyl-2-pyrazolines. The Lipinski profiles and calculated ADME properties of the compounds are also reported.

Solution-Phase Parallel Synthesis of a Library of ¢2-Pyrazolines

Request more information about Solution-Phase Parallel Synthesis of a Library of ¢2-Pyrazolines...

Applications

• Novel parallel synthesis of N-(4-oxo-2-substituted-4H-quinazolin-3-yl)-substituted sulfonamides
• Use of Quinolinium Salts in Parallel Synthesis for the Preparation of 4-Amino-2-alkyl-1,2,3,4-tetrahydroquinoline
• Parallel Synthesis of 3-Amino-4H-Quinolizin-4-ones, Fused 3-Amino-4H-Pyrimidin-4-ones, and Fused 3-Amino-2H-Pyran-2-ones
• One-Step Synthesis of Oxazoline and Dihydrooxazine Libraries
• Solution-Phase Parallel Synthesis of Hexahydro-1H-isoindolone Libraries via Tactical Combination of Cu-Catalyzed Three-Component Coupling and Diels–Alder Reactions
• Polymer-supported reagents and scavengers to streamline tedious purification steps
• Ionic Immobilization, Diversification, and Release: Application to the Generation of a Library of Methionine Aminopeptidase Inhibitors

• Home
• Application Descriptions
• Solution-Phase Parallel Synthesis of a Library of ¢2-Pyrazolines