16185-96-9Relevant articles and documents
Preparation of Trifluoromethylphenyl Magnesium Halides in the Presence of LiCl and Synthesis of 2′-Trifluoromethyl-Aromatic Ketones
Nakatani, Jiro,Nozoe, Tatsuhiro
, p. 1633 - 1636 (2016)
The effect of LiCl-promoted insertion of magnesium turnings into halogenated-trifluoromethylbenzenes for Grignard reagent synthesis was investigated. In the presence of less than 1.0 equiv of LiCl, chloro(trifluoromethyl)benzene Grignard reagents were easily generated. The 2-trifluoromethylphenyl magnesium chloride Grignard reagent was obtained in high yield and 2′-trifluoromethyl-substituted aromatic ketone was synthesized through reaction of the obtained Grignard reagent with a carboxylic anhydride in an 83% yield.
METHOD OF PRODUCING 2'-TRIFLUOROMETHYL GROUP-SUBSTITUTED AROMATIC KETONE
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Paragraph 0042; 0043; 0044; 0045; 0048; 0052, (2017/04/18)
A method produces a 2′-trifluoromethyl-substituted aromatic ketone and includes reacting a 2-halogen-substituted benzotrifluoride compound with magnesium metal to convert the compound to a Grignard reagent; and reacting the Grignard reagent with an acid anhydride; and then hydrolyzing the resultant to produce a 2′-trifluoromethyl-substituted aromatic ketone. The method of producing a 2′-trifluoromethyl-substituted aromatic ketone enables 2′-trifluoromethyl-substituted aromatic ketone to be produced without using expensive raw materials by generating a Grignard reagent as an intermediate and reacting this Grignard reagent with an acid anhydride in an efficient productivity. The 2′-trifluoromethyl-substituted aromatic ketone that is produced by the method of producing a 2′-trifluoromethyl-substituted aromatic ketone can be used as fine chemicals, raw materials for pharmaceuticals and agrochemicals, raw materials for resins and plastics, electronics and information related materials, optical materials, and the like.
Synthesis and activity of 2-methyl-3-aminopropiophenones as centrally acting muscle relaxants
Shiozawa,Narita,Izumi,Kurashige,Sakitama,Ishikawa
, p. 85 - 94 (2007/10/02)
Some novel 2-methyl-3-aminopropiophenones were synthesized and their centrally acting muscle relaxant activities were,evaluated for an inhibitory effect on the flexor reflex in rats. The structure-activity relationships are discussed. In this series 2-methyl-3-pyrrolidino-1-(4-trifluoromethylphenyl)-propan-1-one (28) showed significant centrally acting muscle relaxant activity. In addition, the activities of each enantiomer (28-(S) and (R)) were studied along with their acute toxicities. Compound 28-(R) was found to exhibit more potent activity and weaker acute toxicity than 28-(S). Accordingly, compound 28-(R) (NK433) is under development as a novel centrally acting muscle relaxant.