4-(Isoxazol-3-yl)pyrimidines from Pyrimidinyl Nitrile Oxides

The 1,3-dipolar cycloaddition reaction of pyrimidinyl aldoxime derived nitrile oxides and alkynes delivers 4-(isoxazol-3-yl)pyrimidines. The procedures reported accommodate three points of diversification around this bisheterocyclic scaffold and the resulting library of compounds has been added to t...

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Bibliographic Details
Published inSynlett no. 19; pp. 3036 - 3040
Main Authors Choung, Wonken, Lorsbach, Beth A., Sparks, Thomas C., Ruiz, James M., Kurth, Mark J.
Format Journal Article
LanguageEnglish
Published STUTTGART Thieme Medical Publishers 01.12.2008
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
isoxazolines
KETONES
cycloaddition
ACIDS
isoxazoles
INHIBITORS
ipso substitution
nitrile oxide
DISCOVERY
2-aminopyrimidine
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Summary:The 1,3-dipolar cycloaddition reaction of pyrimidinyl aldoxime derived nitrile oxides and alkynes delivers 4-(isoxazol-3-yl)pyrimidines. The procedures reported accommodate three points of diversification around this bisheterocyclic scaffold and the resulting library of compounds has been added to the National Institutes of Health repository (ca. 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.
ISSN:0936-5214
1437-2096
DOI:10.1055/s-0028-1087346