- SUBSTITUTED IMIDAZOLECARBOXYLATE DERIVATIVES AND THE USE THEREOF
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A compound is shown in formula (I). The derivatives of the compound include a stereoisomer, a pharmaceutically acceptable salt, a solvate, a prodrug, a metabolite, a deuterated derivative. The compound is a structurally novel substituted imidazole formate derivative. Substituted imidazole formate derivatives are used in preparing a drug with sedative, hypnotic and/or anesthetic effects, as well as a drug that can control the state of epilepsy. The compound has a good inhibitory effect on the central nervous system, and provides a new option for clinical screening of and/or preparation of a drug with sedative, hypnotic and/or anesthetic effects and controlling the state of epilepsy.
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Paragraph 0912-0914; 1003-1004
(2020/12/08)
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- Diastereo- and enantioselective iridium-catalyzed carbonyl propargylation from the alcohol or aldehyde oxidation level: 1,3-enynes as allenylmetal equivalents
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Axial to axial to point chirality transfer: Exposure of conjugated enynes to alcohols in the presence of an iridium catalyst modified by a segphos ligand results in the generation of aldehyde-allenyliridium pairs and formation of enantiomerically enriched products of carbonyl anti-(α-methyl) propargylation (see scheme). An identical set of products are obtained from aldehydes under related transfer hydrogenation conditions by employing formic acid as a reductant. Copyright
- Geary, Laina M.,Woo, Sang Kook,Leung, Joyce C.,Krische, Michael J.
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supporting information; experimental part
p. 2972 - 2976
(2012/04/18)
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- Ruthenium-catalyzed reductive coupling of 1,3-enynes and aldehydes by transfer hydrogenation: Anti-diastereoselective carbonyl propargylation
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Under the conditions of ruthenium-catalyzed transfer hydrogenation employing isopropanol as a source of hydrogen, isopropoxy-substituted enyne 1 b and aldehydes 3 a-3 l engage in reductive coupling to provide products of propargylation 4 a-4 l with good to complete levels of anti- diastereoselectivity. The unprotected tertiary hydroxy moiety of isopropoxy enyne 1 b is required to enforce diastereoselectivity. Deuterium-labeling studies corroborate reversible enyne hydrometalation in advance of carbonyl addition. As demonstrated in the conversion of 4 f-h and 4 k to 5 f-h and 5 k, the isopropoxy group of the product is readily cleaved upon exposure to aqueous sodium hydroxide to reveal the terminal alkyne. Unprotected coupling is better! Ruthenium-catalyzed transfer hydrogenation of enynes in the presence of aldehydes promotes reductive C-C coupling to provide products of propargylation with good to complete levels of anti-diastereoselectivity (see scheme). The unprotected hydroxy group of the isopropoxy-substituted enyne is required to enforce high levels of anti-diastereoselectivity. Copyright
- Geary, Laina M.,Leung, Joyce C.,Krische, Michael J.
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supporting information
p. 16823 - 16827
(2013/03/28)
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- Direct N- and C-vinylation with trimethoxyvinylsilane
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Treatment of nucleobases, nucleosides, 5-membered N-heterocycles and terminal alkynes with trimethoxyvinylsilane in the presence of copper(II) acetate-TBAF system as catalyst affords the vinylation products.
- Arsenyan, Pavel,Petrenko, Alla,Paegle, Edgars,Belyakov, Sergey
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experimental part
p. 326 - 328
(2012/02/04)
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- Regiocontrol of the palladium-catalyzed tin hydride addition to Z-enynols: Remarkable Z-directing effects
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(Figure Presented) Palladium-catalyzed hydrostannation of substituted Z- and E-enynols is discussed and compared. The regioselectivity of the H-Sn bond addition was found to be controlled by the geometry of the double bond (Z- or syn-directing effect) rather than the nature of its substituents, Exclusively α-vinyl stannanes were obtained from Z-enynols having various substituents on the double bond regardless of their electronic, steric, or chelating natures.
- Hamze, Abdallah,Provot, Olivier,Brion, Jean-Daniel,Alami, Mouad
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p. 3868 - 3874
(2008/02/02)
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- Hydrazines and azides via the metal-catalyzed hydrohydrazination and hydroazidation of olefins
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The discovery, study, and implementation of the Co- and Mn-catalyzed hydrohydrazination and hydroazidation reactions of olefins are reported. These reactions are equivalent to direct hydroaminations of C-C double bonds with protected hydrazines or hydrazoic acid but are based on a different concept in which the H and the N atoms come from two different reagents, a silane and an oxidizing nitrogen source (azodicarboxylate or sulfonyl azide). The hydrohydrazination reaction using di-tert-butyl azodicarboxylate is characterized by its ease of use, large functional group tolerance, and broad scope, including mono-, di-, tri-, and tetrasubstituted olefins. Key to the development of the hydroazidation reaction was the use of sulfonyl azides as nitrogen sources and the activating effect of tert-butyl hydroperoxide. The reaction was found to be efficient for the functionalization of mono-, di-, and trisubstituted olefins, and only a few functional groups are not tolerated. The alkyl azides obtained are versatile intermediates and can be transformed to the free amines or triazoles without isolation of the azides. Preliminary mechanistic investigations suggest a rate-limiting hydrocobaltation of the alkene, followed by an amination reaction. Radical intermediates cannot be ruled out and may be involved.
- Waser, Jerome,Gaspar, Boris,Nambu, Hisanori,Carreira, Erick M.
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p. 11693 - 11712
(2007/10/03)
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- Cobalt-catalyzed hydrohydrazination of dienes and enynes: Access to allylic and propargylic hydrazides
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(Chemical Equation Presented) The cobalt-catalyzed hydrohydrazination reaction of dienes and enynes is presented. Allylic and propargylic hydrazines were obtained in synthetically useful yields (allylic amines, 60-90%; propargylic amines, 47-83%) and good chemo- and regioselectivity.
- Waser, Jerome,Gonzalez-Gomez, Jose C.,Nambu, Hisanori,Huber, Pascal,Carreira, Erick M.
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p. 4249 - 4252
(2007/10/03)
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