126536-03-6Relevant articles and documents
1-Alkyl-2-trifluoromethylaziridines: The bacisity and ring-opening reactions under the action of acids
Karimova,Teplenicheva,Kolomiets,Fokin
, p. 1136 - 1139 (1997)
The basicity of 1-alkyl-2-trifluoromethylaziridines is -two orders of magnitude lower than that of non-fluorinated analogs. Aziridines are stable to H2S and AcOH, but react with AcSH, HCl, HBr, H2SO4, TsOH, and picric acid to give products of ring-opening.
Synthesis of 2- and 3-trifluoromethylmorpholines: Useful building blocks for drug discovery
Shcherbatiuk, Andriy V.,Shyshlyk, Oleg S.,Yarmoliuk, Dmytro V.,Shishkin, Oleg V.,Shishkina, Svitlana V.,Starova, Viktoriia S.,Zaporozhets, Olga A.,Zozulya, Sergey,Moriev, Roman,Kravchuk, Olga,Manoilenko, Olga,Tolmachev, Andrey A.,Mykhailiuk, Pavel K.
, p. 3796 - 3804 (2013/07/05)
2- and 3-Trifluoromethylmorpholines were prepared in racemic and optically active forms. The synthesis commenced from the commercially available 2-trifluoromethyloxirane. The elaborated procedures were scalable, and the products were obtained in multigram quantities. The obtained compounds were comprehensively characterized by crystallographic analysis, fluorescence measurements, solubility, pKa, logD parameters, and clearance rate. The potential of the synthesized amines as the building blocks for drug discovery is thus demonstrated.
