Abstract
The solution-phase parallel synthesis of a 136-member library of isoxazol(in)e-CH2-pyrazoles is described, X-ray crystallographic structure determination verified the regioselectivities of the N-alkylation and nitrile oxide 1,3-dipolar cycloaddition steps. The construction of these pharmaceutically relevant heterocycles on solid support under microwave irradiation is also demonstrated. The resulting library of drug-like compounds has been added to the National Institutes of Health repository (∼10 mg of each with ≥90% purity) for pilot-scale biomedical studies with bioassay data available at the National. Center for Biotechnology Information PubChem database. A subset of these compounds has been broadly screened by Dow AgroSciences for herbicidal, fungicidal, and insecticidal activity.
Original language | English (US) |
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Pages (from-to) | 129-136 |
Number of pages | 8 |
Journal | Journal of Combinatorial Chemistry |
Volume | 12 |
Issue number | 1 |
DOIs | |
State | Published - Jan 11 2010 |
ASJC Scopus subject areas
- Chemistry(all)