- ARYLCYCLOHEXYLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PSYCHIATRIC DISORDERS
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Provided herein are arylcyclohexylamine derivatives and their use in the treatment of psychiatric disorders.
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Paragraph 0311
(2021/07/02)
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- Chromium(II)-Catalyzed Diastereoselective and Chemoselective Csp2-Csp3 Cross-Couplings Using Organomagnesium Reagents
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A simple protocol for performing chromium-catalyzed highly diastereoselective alkylations of arylmagnesium halides with cyclohexyl iodides at ambient temperature has been developed. Furthermore, this ligand-free CrCl2 enables efficient electrophilic alkenylations of primary, secondary, and tetiary alkylmagnesium halides with readily available alkenyl acetates. Moreover, this chemoselective C-C coupling reaction with stereodefined alkenyl acetates proceeds in a stereoretentive fashion. A wide range of functional groups on alkyl iodides and alkenyl acetates are well tolerated, thus furnishing functionalized Csp2-Csp3 coupling products in good yields and high diastereoselectivity. Detailed mechanistic studies suggest that the in situ generated low-valent chromium(I) species might be the active catalyst for these Csp2-Csp3 cross-couplings.
- Li, Jie,Ren, Qianyi,Cheng, Xinyi,Karaghiosoff, Konstantin,Knochel, Paul
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supporting information
p. 18127 - 18135
(2019/11/19)
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- BIARYL PYRAZOLES AS NRF2 REGULATORS
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The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
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Page/Page column 463
(2017/08/01)
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- SYNTHESIS METHOD FOR L-CYCLIC ALKYL AMINO ACID AND PHARMACEUTICAL COMPOSITION HAVING THEREOF
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A synthesis method for L-cyclic alkyl amino acid and a pharmaceutical composition having the said amino acid are provide in the present disclosure provides. The synthesis method comprises: step A.) preparing a cyclic alkyl keto acid or a cyclic alkyl keto acid salt having Structural Formula (I) or Structural Formula (II), and step B.) mixing the cyclic alkyl keto acid or the cyclic alkyl keto acid salt with ammonium formate, a leucine dehydrogenase, a formate dehydrogenase and a coenzyme NAD+, and carrying out a reductive amination reaction to generate the L-cyclic alkyl amino acid, wherein the Structural Formula (I) is where n1≧1, m1≧0 and the M1 is H or a monovalent cation; the Structural Formula (II) is where n2≧0, m2≧0, the M2 is H or a monovalent cation, an amino acid sequence of the leucine dehydrogenase is SEQ ID No.1.
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Paragraph 0066-0067
(2016/11/17)
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- METHOD FOR PREPARING DI-ORGANO-DIALKOXYSILANES
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The present invention relates to a method for preparing di-organo-dialkoxysilanes, in particular di-organo-dialkoxysilanes wherein one or both of the organic substituents are bulky. The method comprises reacting a tetraalkoxysilane compound with a first Grignard reagent to form a mono-organo-tri-alkoxysilane compound, which is then reacted with a chlorinating agent to form a chlorinated mono-organo-di-alkoxysilane which is then reacted with a second Grignard reagent to form the di-organo-di-alkoxysilane compound.
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Paragraph 0060
(2013/07/19)
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- PYRIDO [4,3-B] INDOLES AND METHODS OF USE
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New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
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Page/Page column 86
(2010/11/17)
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- Absolute kinetic rate constants and activation energies for the formation of Grignard reagents
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This paper reports the first absolute rate constants for the formation of Grignard reagents from magnesium metal and organohalides. The theory that allows calculation of heterogeneous rate constants from the rate of growth of individual pits is described. By monitoring the reaction of individual reactive sites on the magnesium surface using photomicrography, it is possible to determine the rate of reaction and the active surface area; rate constants then are calculated from those data. Rate constants are on the order of 10-4 cm/s and vary relatively little between various organohalides. By measuring rate constants over a range of temperatures, Arrhenius parameters are determined for the reaction. The magnitudes of the enthalpic and entropic barriers are not consistent with electron transfer as the rate-limiting step. Rather, the data suggest that the rate-limiting step is reaction of the organohalide at the magnesium surface with partial insertion of a magnesium atom into the carbon-halide bond in the transition state.
- Beals, Bridget J.,Bello, Zainab I.,Cuddihy, Kathleen P.,Healy, Ethan M.,Koon-Church, Stephanie E.,Owens, Jane M.,Teerlinck, Cynthia E.,Bowyer, Walter J.
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p. 498 - 503
(2007/10/03)
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- Thermochemical Bond Dissociation Energies of Carbon-Magnesium Bonds
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The heats of formation of 29 alkylmagnesium bromides, isobutyl bromide, and neopentyl bromide have been determined, and bond dissociation energies have been derived for the Grignard reagents.For saturated alkyl derivatives the C-Mg bond strength decreases with an increasing number of β-hydrogens in the series methyl, neopentyl, isobutyl, butyl, ethyl, 1-ethylpropyl, 1-methylpropyl, isopropyl, and t-butyl.Bonding in alkyl bromides and alkylmagnesium bromides is discussed.
- Holm, Torkil
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p. 464 - 467
(2007/10/02)
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- Mechanism of Formation of Grignard Reagents. Rate of Reaction of Cyclopentyl Bromide with a Rotating Disk of Magnesium
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Careful studies of the dependence of the rate of reaction (k) of cyclopentyl bromide in diethyl ether with the surface of rotating disk as a function of the angular lelocity (ω) of the disk confirm the relation k * ω1/2 expected for a mass-transfer limited reaction.More limited studies also indicate that the variations in this rate with other parameters are compatible with those expected for a mass-transfer limited reaction: k * (η)-5/6(ρ)1/6 (η is the shear viscosity of the solution and ρ is its density); k * D2/3 (D is the diffusion coefficient of the alkyl halide).
- Root, Karen S.,Deutch, John,Whitesides, George M.
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p. 5475 - 5479
(2007/10/02)
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