177965-07-0Relevant academic research and scientific papers
Catalytic asymmetric synthesis of new halogenated chiral synthons
Vanhessche, Koen P. M.,Sharpless, K. Barry
, p. 517 - 522 (1997)
Two-step and practical asymmetric syntheses of enantiomerically pure 4-trifluoromethyl-2.2-dioxo-1,3,2-dioxathiolane and 4-trichloromethyl-2,2-dioxo-1,3,2-dioxathiolane (>98% ee) have been achieved. Catalytic asymmetric dihydroxylation (AD) of 3,3,3-trifl
GCN2 INHIBITORS AND USES THEREOF
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Paragraph 00646; 00647, (2019/08/12)
The present invention provides compounds, compositions thereof, and methods of using the same.
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.
Optical purifications via self-disproportionation of enantiomers by achiral chromatography: Case study of a series of α-CF3-containing secondary alcohols
Sorochinsky, Alexander E.,Katagiri, Toshimasa,Ono, Taizo,Wzorek, Alicja,Acena, Jose Luis,Soloshonok, Vadim A.
, p. 365 - 368 (2013/07/27)
This work demonstrates that self-disproportionation of enantiomers via achiral chromatography can be recommended as inexpensive and general method for optical purification of enantiomerically enriched compounds. In particular, the advantage of this approach over conventional recrystallization is that it can be used for both crystalline as well as liquid compounds.
Intramolecular S(N)2 reaction at α-carbon of trifluoromethyl group: Preparation of optically active 2-trifluoromethylaziridine
Katagiri, Toshimasa,Ihara, Hideki,Takahashi, Mikihiro,Kashino, Setsuo,Furuhashi, Keizo,Uneyama, Kenji
, p. 2933 - 2937 (2007/10/03)
We have succeeded in intramolecular nucleophilic substitution of the hydroxyl group in (S)-1-(alkylamino)-3,3,3-trifluoro-2-propanol. The reaction provides an optically pure (R)-1-benzyl-2-trifluoromethylaziridine in good yield from optically pure (S)-3-(benzylamino)-1,1,1-trifluoro-2-propanol which was prepared from (S)-3,3,3-trifluoropropene oxide (75% ee).
