Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 15, Issue 5, Pages 1228-1235Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6ob02137a
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Funding
- National Program on Key Research Project [2016YFA0602900]
- National Natural Science Foundation of China [21472051, 21420102003]
- Guangdong Natural Science Foundation [2016A030310460]
- Fundamental Research Funds for the Central Universities [2015ZY001, 2015ZM163]
- China Postdoctoral Science Foundation [2015M580717]
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A palladium-catalyzed cyclopropanation of internal alkenes with N-tosylhydrazones is presented. This gram-scale cyclopropanation reaction of maleimides provides a wide spectrum of 3-azabicyclo[3.1.0]hexane derivatives in high yields and diastereoselectivities. The major diastereoisomers could be easily isolated by chromatography on silica gel. This protocol provides a practical route to the mu opioid receptor antagonist CP-866,087.
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