- ION CHANNEL MODULATORS
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The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
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Page/Page column 59
(2021/06/04)
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- Process for producing optically active aliphatic fluoroalcohol
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The problem to be resolved by the present invention is to provide a method for efficiently synthesizing optically active lower aliphatic alcohols that have difficulty in separation from organic solvents, without using a special reactor. The present invention relates to a method for producing an optically active aliphatic alcohol having a fluorine atom at α position, wherein an optically active alcohol is produced by reacting an aliphatic ketone having a fluorine atom at α position in water using a formate, under the presence of an asymmetric catalyst represented by general formula (1) and an acid.
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Page/Page column 14
(2012/01/11)
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- Study for the determination of the absolute configuration of fluoromethylated secondary alcohols by the modified Mosher method
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Application of the modified Mosher method using high-field FT 1H NMR to the 2-methoxy-2-phenyl-2-trifluoromethyl acetic acid (MTPA) derivatives of fluorinated secondary alcohols indicates that this method may be generally used to determine the absolute configurations of these materials.
- Xiao, Ling,Yamazaki, Takashi,Kitazume, Tomoya,Yonezawa, Tetsuo,Sakamoto, Yoshitake,Nogawa, Kouji
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- Deamination Reactions, 43 - The Effect of Trifluoromethyl Groups on the Reactivity of Aliphatic Diazonium Ions and Carbocations
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Various trifluoroalkanamines (9, 26, 35, 38, 45, 56, and 67) have been prepared and diazotized (water, pH 3.5) to probe the effect of trifluoromethyl groups on the reactivity of aliphatic diazonium ions.The product distributions reveal that α-CF3 groups enhance inverting displacement and enforce rearrangement (hydride shifts) separating the positive charge from CF3.Migrations of the positive charge from the β- to the γ-position are less strongly promoted than those from α to β.Enhancement factors of ca. 15 (α -> β) and 4 (β -> γ) may be derived by comparison with analogous alkanediazonium ions.The positive charge does not migrate in the reverse direction (β -> α) except for minor amounts of a pinacolic rearrangement (68 -> 7).A migration of the positive charge from γ to β has been detected with 36 but a tenfold decrease as compared to the analogous butanediazonium ion 37 is indicated.All observations are reasonably explained in terms of the relative stabilities of the intermediate trifluoroalkyl cations.
- Gassen, Karl-Rudolf,Kirmse, Wolfgang
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p. 2233 - 2248
(2007/10/02)
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