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Solution-phase parallel synthesis of a library of delta(2)-pyrazolines
Shankar Manyem1, Mukund P Sibi, Gerald H Lushington
1University of Kansas Center of Excellence in Chemical Methodology and Library Development, Lawrence, Kansas 66047, USA.
None:
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.
