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Quinoline-based compound and selective androgen receptor agonist comprising the same

Provided are a novel quinoline-based compound, a pharmaceutical composition containing the quinoline-based compound, and a method for producing the quinoline-based compound. The quinoline-based compound acts on an androgen receptor to increase activities of the androgen receptor, and thus can be favorably used as an agent for treating and preventing diseases or conditions, in which the increased activities of the androgen can lead to improvement of symptoms or the responsiveness to treatment, for example, various hormone-related diseases of the male or female, muscle-wasting disease, osteoporosis, and the like.COPYRIGHT KIPO 2016

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Discovery of 3340-78-1

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Selective cross-dehydrogenative coupling of N-phenyltetrahydroisoquinolines in aqueous media using poly(aniline sulfonic acid)/gold nanoparticles

Selective cross-dehydrogenative coupling of N-phenyltetrahydroisoquinoline with carbon nucleophiles such as dimethyl malonate, ethyl acetoacetate, and nitromethane was demonstrated in complete aqueous media using poly(2-methoxyaniline-5-sulfonic acid)/gold nanoparticles under molecular oxygen.

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The oxidative Mannich reaction catalyzed by dirhodium caprolactamate

Dirhodium caprolactamate [Rh2(cap)4] is a highly effective catalyst for the oxidative Mannich reaction. The reaction proceeds via C-H oxidation of a tertiary amine followed by nucleophilic capture. This green transformation is conducted in protic solvent using inexpensive T-HYDRO (70% t-BuOOH in water). Synthetically valuable gamma-aminoalkyl butenolides are obtained. Copyright

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CuBr-catalyzed oxidative difluoromethylation of tertiary amines with difluoroenol silyl ethers

CuBr-catalyzed oxidative difluoromethylation of readily available tertiary amines with difluoroenol silyl ethers was performed under mild conditions to afford beta-amine-a,a-difluoro ketones.

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Brief introduction of 118864-75-8

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One-Pot N-Deprotection and Catalytic Intramolecular Asymmetric Reductive Amination for the Synthesis of Tetrahydroisoquinolines

A one-pot N-Boc deprotection and catalytic intramolecular reductive amination protocol for the preparation of enantiomerically pure tetrahydroisoquinoline alkaloids is described. The iodine-bridged dimeric iridium complexes displayed superb stereoselectivity to give tetrahydroisoquinolines, including several key pharmaceutical drug intermediates, in excellent yields under mild reaction conditions. Three additives played important roles in this reaction: Titanium(IV) isopropoxide and molecular iodine accelerated the transformation of the intermediate imine to the tetrahydroisoquinoline product; p-toluenesulfonic acid contributed to the stereocontrol.

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Archives for Chemistry Experiments of 2-Phenyl-1,2,3,4-tetrahydroisoquinoline

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Cobalt-Catalyzed oxidative alpha-cyanation of tertiary aromatic amines with trimethylsilyl cyanide and tert -butyl hydroperoxide

In this Letter is described that a cobalt(II)-tert-butyl hydroperoxide oxidizing system was used to catalyze the alpha-cyanation of aromatic tertiary amines in the presence of trimethylsilyl cyanide to produce the corresponding alpha-aminonitriles in good yields. Georg Thieme Verlag Stuttgart. New York.

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Archives for Chemistry Experiments of 1745-07-9

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Lewis Acid-Catalyzed C(sp3)?C(sp3) Bond Forming Cyclization Reactions for the Synthesis of Tetrahydroprotoberberine Derivatives

An efficient Lewis acid-catalyzed C(sp3)?C(sp3) bond forming annulation reaction has been developed. This strategy serves as a new method for the facile synthesis of tetrahydro-5H-isoquinolino[2,1-g][1,6]naphthyridine derivatives. A wide range of 2-methylquinoline-3-carbaldehydes and 1,2,3,4-tetrahydroisoquinolines can be applied for this process to afford structurally diverse tetrahydroprotoberberine derivatives in excellent yields. (Figure presented.).

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Structure and Mechanism of Titania-Supported Platinum-Molybdenum Catalyst for Hydrodeoxygenation of 2-Furancarboxylic Acid to Valeric Acid

Selective hydrodeoxygenation of 2-furancarboxylic acid, which can be a relatively stable platform chemical from hemicellulose, to valeric acid was investigated in detail, and the reaction has been reported to be specifically promoted by supported Pt-MoOx catalysts. The dependence of catalytic performance of Pt-MoOx/TiO2 on loading amounts of Pt and Mo showed that the highest activity is obtained at around Mo ?0.5 wt % when the Pt loading amount is fixed. With enough of the catalyst that can minimize the effect of deactivation, ?60% yield of valeric acid was obtained over all Pt-MoOx/TiO2 catalysts with Pt ? 1 wt % and 0.5 wt % Mo loadings. Characterization results of Pt-MoOx/TiO2 catalysts with XRD and CO adsorption showed that the Pt particles (3-5 nm, depending on Pt loading amount) were not covered with MoOx species, suggesting that MoOx species were mainly located on the TiO2 support surface. Mo K-edge XAFS results suggest that the MoOx species in Pt-MoOx/TiO2 have a Mo(IV) valence state and some of the MoIVOx species have direct bonds with the Pt atom on Pt metal particles. The number of the direct Pt-Mo bonds became smaller after catalytic use, which can be related to the deactivation. Therefore, the Pt-Mo bimetallic site can be the catalytically active site. Based on the solvent effect, reactivity trends of related substrates, and reaction orders in kinetics, a reaction mechanism is proposed where the ring is opened after addition of one hydrogen atom to the 2-position of the furan ring.

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Tetrahydroisoquinoline – Wikipedia,
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Discovery of 6-Chloro-1,2,3,4-tetrahydroisoquinoline hydrochloride

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DERIVATIVES OF 4-(N-AZACYCLOALKYL) ANILIDES AS POTASSIUM CHANNEL MODULATORS

This invention provides a compound of formula IAwhere X?O or S; Y is O or S; q=1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. They are potentially useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

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Tetrahydroisoquinoline – Wikipedia,
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Discovery of 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

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Method of racemization of optically active tetrahydrofuran-2-carboxylic acid

Disclosed is a method of racemization of optically active tetrahydrofuran-2-carboxylic acid. (+)-Tetrahydrofuran-2-carboxylic acid is useful as a side chain intermediate of the antibiotics of penem series, and is prepared by optical resolution of racemic compound. The remaining (+)-isomer should be racemized and reused as the material for further optical resolution. The racemization can be, in accordance with the present invention, carried out by heating the optically active tetrahydrofuran-2-carboxylic acid to a temperature of 100 C. or higher in the presence of a strong base.

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