Synthesis of Trifluoromethyl-Substituted 3-Azabicyclo[n.1.0]alkanes: Advanced Building Blocks for Drug Discovery

Five CF3‐substituted 3‐azabicyclo[n.1.0]alkanes were synthesized by CuCl‐mediated trifluoromethylcyclopropanation reaction of the corresponding cyclic enamides with CF3CHN2. A mini‐library of CF3‐substituted bicyclic amines has been synthesized by using CF3CHN2.

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Bibliographic Details
Published in:European journal of organic chemistry 2014-06, Vol.2014 (17), p.3592-3598
Main Authors: Artamonov, Olexiy S., Slobodyanyuk, Evgeniy Y., Volochnyuk, Dmitriy M., Komarov, Igor V., Tolmachev, Andrey A., Mykhailiuk, Pavel K.
Format: Article
Language:English
Subjects:
Drug discovery
Fluorine
Nitrogen heterocycles
Synthetic methods
Trifluoromethyldiazomethane
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Description
Summary:Five CF3‐substituted 3‐azabicyclo[n.1.0]alkanes were synthesized by CuCl‐mediated trifluoromethylcyclopropanation reaction of the corresponding cyclic enamides with CF3CHN2. A mini‐library of CF3‐substituted bicyclic amines has been synthesized by using CF3CHN2.
ISSN:1434-193X
1099-0690
DOI:10.1002/ejoc.201402158