期刊
ORGANIC LETTERS
卷 21, 期 14, 页码 5432-5437出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b01650
关键词
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资金
- National Natural Science Foundation of China [21871045, 21831002]
- Natural Science Foundation of Jilin Province [20160519003JH, 20190201070JC]
- Changbai Mountain Scholarship Program
- Fundamental Research Funds for the Central Universities [2412017FZ014]
The use of functional-group-tolerant organo-boron in lieu of basic organometallic reagents in base-metal catalyzed cyclopropene carbometalation opens three-component cyclopropane synthesis, as exemplified by the modular assembly of the highly medicinally relevant 2-arylcyclopropylamine (ACPA) framework via stereoselective carboamination. The highly enantioselective version has been realized to afford enantioenriched ACPAs with up to all three cyclopropyl carbons as stererogenic centers in one operation, representing the first example of enantioselective multicomponent cyclopropane synthesis. The reaction significantly improves the efficiency of ACPA synthesis and may inspire the development of other multicomponent cyclopropane syntheses beyond amination.
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