期刊
ORGANIC LETTERS
卷 17, 期 8, 页码 1938-1941出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b00641
关键词
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资金
- Institute for Basic Science [IBS-R010-G1]
- Ministry of Science, ICT & Future Planning, Republic of Korea [IBS-R010-D1-2015-A00] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
C2- and C5-alkynylated quinolone scaffolds are core structures of numerous biologically active molecules. Utilizing TIPS-EBX as an alkynylating agent, we have developed an efficient and site-selective C5 alkynylation of 4-quinolones that is directed by the weakly coordinating carbonyl group. In addition, Ru(II) catalyzed C2-selective alkynylation was successfully realized via N-pyrimidyl group-directed cross-couplings to access valuable C2-alkynylated 4-quinolones. This strategy provides direct access to the C2 or C5 alkynylated 4-quinolones. Furthermore, the reaction was applied to isoquinolones for C3-selective alkynylation.
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