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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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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.
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creator Artamonov, Olexiy S.
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description 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.
doi_str_mv 10.1002/ejoc.201402158
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subjects Drug discovery
Fluorine
Nitrogen heterocycles
Synthetic methods
Trifluoromethyldiazomethane
title Synthesis of Trifluoromethyl-Substituted 3-Azabicyclo[n.1.0]alkanes: Advanced Building Blocks for Drug Discovery
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