期刊
ORGANIC LETTERS
卷 22, 期 17, 页码 6868-6872出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c02408
关键词
-
资金
- Ministry of Science and Technology of the Republic of China [MOST 107-2628-M-003-001-MY3]
An efficient method for the direct ss-acylation of arylidene pyrazolones and thiazolones with acyl chlorides in the presence of a base catalyzed by organophosphanes is reported. A variety of functionalized 4-arylidene pyrazolone and 5-arylidene thiazolone derivatives were prepared under metal-free and mild conditions via a tandem phospha-Michael addition/O-acylation/intramolecular cyclization/rearrangement sequence. Our mechanistic investigations revealed that the reaction is highly stereospecific to provide exclusively cis-isomers, and the methodology can also be scaled up with similar efficacy.
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