期刊
ORGANIC LETTERS
卷 17, 期 10, 页码 2454-2457出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b00960
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资金
- MEXT
- JST (ACT-C)
- JSPS
- Grants-in-Aid for Scientific Research [14J05174] Funding Source: KAKEN
A sequential procedure for the synthesis of 2,5-disubstituted thiazoles from terminal alkynes, sulfonyl azides, and thionoesters is reported. A copper(I)-catalyzed 1,3-dipolar cycloaddition of terminal alkynes with sulfonyl azides affords 1-sulfonyl-1,2,3-triazoles, which then react with thionoesters in the presence of a rhodium(II) catalyst The resulting 3-sulfonyl-4-thiazolines subsequently aromatize into the corresponding 2,5-disubstituted thiazoles by elimination of the sulfonyl group.
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