Abstract
A concise synthetic route to physostigmine has been developed, where the key step relies on the alkylative cyclization of 1,3-dimethylindole with (Z)-aziridine catalyzed by Sc(OTf)3 and TMSCI in dichloromethane at -30 degrees C, to give 8 in 90% yield, which, in turn, can be readily converted into physostigmine.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkylation
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Aziridines / chemistry*
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Cholinesterase Inhibitors / chemical synthesis*
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Cyclization
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Indicators and Reagents
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Physostigmine / chemical synthesis*
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Skatole / chemistry*
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Solvents
Substances
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Aziridines
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Cholinesterase Inhibitors
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Indicators and Reagents
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Solvents
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Physostigmine
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Skatole