期刊
TETRAHEDRON LETTERS
卷 60, 期 39, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2019.151061
关键词
C-H acylation; Thioester; Liebeskind-Srogl reaction; Indole-indolone scaffolds
资金
- Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Youth Innovation Promotion Association CAS [2014229, 2018293]
- Institutes for Drug Discovery and Development, Chinese Academy of Sciences [CASIMM0120163006]
- Science and Technology Commission of Shanghai Municipality [17JC1405000]
- Program of Shanghai Academic Research Leader [19XD1424600]
- National Science AMP
- Technology Major Project Key New Drug Creation and Manufacturing Program, China [2018ZX09711002-006]
- State Key Laboratory of Natural and Biomimetic Drugs
- NSFC [21772211]
A palladium-catalyzed intramolecular C-H acylation of indole with thioester is described, providing a direct and effective approach for the synthesis of the biologically active indole-indolone scaffolds. The method obviates the need for the prefunctionalized starting materials including organometallic reagents, alkyl halides, and NHP esters in previous metal-catalyzed cross-coupling reaction with thioester. Substrates bearing sensitive halo groups are compatible in the reaction, leaving a functional handle for further structural elaborations. (C) 2019 Elsevier Ltd. All rights reserved.
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