- BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF ROR-GAMMA
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Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
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Paragraph 00238-00239
(2017/08/21)
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- Organolithium-induced alkylative ring opening of aziridines: Synthesis of unsaturated amino alcohols and ethers
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Organolithium-induced alkylative ring opening of N-sulfonyl-protected aziridinyl ethers is described. The reactions were efficiently carried out with a variety of organolithiums, providing a promising new strategy to unsaturated amino alcohols and ethers.
- Hodgson, David M.,Stefane, Bogdan,Miles, Timothy J.,Witherington, Jason
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p. 8510 - 8515
(2007/10/03)
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- Catalysis by ionic liquid. A green protocol for the stereoselective debromination of vicinal-dibromides by [pmIm]BF4 under microwave irradiation
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An easily accessible ionic liquid, 1-methyl-3-pentylimidazolium fluoroborate, [pmIm]BF4, has been demonstrated to be an efficient catalyst as well as reaction medium for the stereoselective debromination of a variety of structurally diverse vicinal-dibromides to the corresponding (E)-alkenes in high yields under microwave irradiation. This reaction does not require any organic solvent and any metal or any conventional reducing agent, and the ionic liquid is recycled without any appreciable loss of its catalytic efficiency.
- Ranu, Brindaban C.,Jana, Ranjan
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p. 8621 - 8624
(2007/10/03)
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- Dichloroindium hydride (Cl2InH): A convenient reagent for stereoselective reduction of vic-dibromides to (E)-alkenes
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Dichloroindium hydride (Cl2InH) generated in situ from the combination of a catalytic amount of indium(III) chloride and sodium borohydride in acetonitrile reduces activated vic-dibromides to the corresponding (E)-alkenes in excellent yields.
- Ranu, Brindaban C.,Das, Arijit,Hajra, Alakananda
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p. 1012 - 1014
(2007/10/03)
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- A new route to amino-2-propanol structures with adrenergic β-blocker activity using low valent titanium
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Amino-2-propanol structures can be obtained by addition to dibenzyl acetals of in situ generated dihalocarbenes using LTV (Low Valent Titanium). This methodology can be used to obtain adrenergic β-blockers with amino-2-propanol structure. Tetrahalomethane are the best dihalocarbene precursors. The yields obtained using halofluromethanes can be increased by addition of carbontetrachloride. A process that can imply halogen transfer may be proposed.
- Bermudez,Del Campo,Sinisterra,Llama
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p. 4137 - 4140
(2007/10/03)
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- Preparation of dialkoxybutenes
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Dialkoxybutenes are selectively prepared in high yields by reacting 1,3-butadiene with an alcohol in the presence of oxygen and a catalytically effective amount of solid particulates which comprise a catalytically active phase deposited onto particles of a support therefor, such catalytically active phase comprising at least one Group VIII noble metal first component, at least one tellurium, selenium and/or sulfur second component, and, optionally, at least one bismuth, antimony, copper and/or tin third component.
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- Carbonylation of allylic ethers to esters
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A method is disclosed for the production of esters by reaction of an allylic ether with carbon monoxide in the presence of a catalytically effective amount of a Group VIII noble metal catalyst and halide compound to obtain esters. The halide compound is present in an amount sufficient to prevent the catalyst from being converted into a Group VIII metal during the reaction. When the reaction is conducted in the presence of a quaternary ammonium salt the ester may be extracted by solvent extraction to minimize catalyst decomposition caused when extractive distillation is used to separate the ester.
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