106240-89-5Relevant academic research and scientific papers
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.
Straightforward synthesis of 1-alkyl-2-(trifluoromethyl)aziridines starting from 1,1,1-trifluoroacetone
Kenis, Sara,D'Hooghe, Matthias,Verniest, Guido,Nguyen, Vinh Duc,Thi, Tuyet Anh Dang,Nguyen, Tuyen Van,Kimpe, Norbert De
, p. 7217 - 7223 (2011/11/06)
An efficient and straightforward approach towards the synthesis of 1-alkyl-2-(trifluoromethyl)aziridines starting from 1,1,1-trifluoroacetone via imination, α-chlorination, hydride reduction and ring closure was developed. In addition, novel primary β-iodo amines were obtained by regioselective ring opening of these 2-(trifluoromethyl)aziridines using alkyl iodides, and their synthetic potential was demonstrated by converting them into novel α-CF3-β-phenylethylamines upon treatment with lithium diphenylcuprate.
Preparation and reactions of (β-trifluoromethyl)vinyl sulfonium salt
Maeda, Ryoko,Ooyama, Kyoko,Anno, Ryoko,Shiosaki, Masahiro,Azema, Takayuki,Hanamoto, Takeshi
supporting information; experimental part, p. 2548 - 2550 (2010/07/20)
(β-Trifluoromethyl)vinyl sulfonium salt as a novel three-carbon fluorinated building block was conveniently prepared from easily available (β-trifluoromethyl)vinyl sulfide and diphenyl iodonium salt in excellent yield. This easily handled crystalline reag
Electronic structure and reactivity of organofluorine compounds 6. The effect of the position of the CF3 group on the basicity of aliphatic amines
Rozhkov, I.N.,Karimova, N. M.,Ignatova, Yu. L.,Matveeva, A. G.
, p. 258 - 260 (2007/10/02)
The basicity of isomeric bromoethylamines having a CF3 substutient in the α- and β-positions with respect to the amino group was studied.According to potentiometric titration in H2O, CH3NO2, and CH3CN, the basicity of α-trifluoromethylamines is 4-5 orders
