期刊
JOURNAL OF COMBINATORIAL CHEMISTRY
卷 10, 期 4, 页码 521-525出版社
AMER CHEMICAL SOC
DOI: 10.1021/cc800033m
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资金
- NIGMS NIH HHS [GM076151] Funding Source: Medline
Condensation of 3-chloropentane-2,4-dione with thioamides gives 1-(thiazol-5-yl)ethanones and subsequent Wittig olefination, followed by nitrile oxide 1,3-dipolar cycloaddition to the resulting prop-l-en-2-yl moiety, delivers racemic 5-(thiazol-5-yl)-4,5-dihydroisoxazoles. When this thiazole and isoxazoline diheterocyclic scaffold has a carboethoxy substituent at C2 of the thiazole ring, aminolysis provides for effective diversification. A 50-member library of various 5-(thiazol-5-yl)-4,5-dihydroisoxizoles is reported.
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