- 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 0927-0929
(2020/12/08)
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- Visible-light-driven selective alkenyl C-P bond cleavage of allenylphosphine oxides
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An efficient method for highly selective alkenyl C-P bond cleavage, enabled by organic dyes and visible-light irradiation, was developed. This novel protocol involves a highly regioselective radical pathway initiated by singlet oxygen, affording diverse a
- Wei, Kai,Luo, Kai,Liu, Fang,Wu, Lei,Wu, Li-Zhu
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supporting information
p. 1994 - 1998
(2019/03/29)
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- Synthesis of 4-Oxoisoxazoline N-Oxides via Pd-Catalyzed Cyclization of Propargylic Alcohols with tert-Butyl Nitrite
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A cyclization of propargylic alcohols with tert-butyl nitrite at room temperature in air was achieved using Pd(OAc)2 as catalyst. The first reported 4-oxoisoxazoline N-oxides could be directly accessed from a range of multisubstituted propargylic alcohols in moderate to excellent yields under mild conditions. Density functional theory calculations indicated that the reaction proceeds through a palladium-catalyzed NO2 addition that efficiently generates a ketoxime radical, which eventually produces 4-oxoisoxazoline N-oxide.
- Feng, Kai-Wen,Ban, Yong-Liang,Yuan, Pan-Feng,Lei, Wen-Long,Liu, Qiang,Fang, Ran
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supporting information
p. 3131 - 3135
(2019/05/10)
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- Transition Metal Free Cycloamination of Prenyl Carbamates and Ureas Promoted by Aryldiazonium Salts
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Upon treatment with aryldiazonium salts, prenyl carbamates and ureas undergo redox-neutral azocycloamination. In general, N-aryl O-prenyl carbamates cyclize in a photocatalytic reaction with visible light and an organic dye. With electron-deficient diazonium salts, electronic matching with an electron-rich N-aryl substituent results in a reaction proceeding in the ground state, without either light or photocatalyst. Cyclic voltammetry suggests that this radical reaction is initiated by hydrogen-atom abstraction mediated by an aryl radical, followed by a radical addition cascade and proton-coupled hole propagation. The reaction proceeds at room temperature in short reaction times, and a range of functional groups is tolerated.
- Abrams, Roman,Lefebvre, Quentin,Clayden, Jonathan
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supporting information
p. 13587 - 13591
(2018/09/25)
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- Palladium-Catalyzed Cascade C?O Cleavage and C?H Alkenylation of Phosphinyl Allenes: An Expeditious Approach to 3-Alkenyl Benzo[b]phosphole Oxides
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A phosphine oxide-directed intramolecular cyclization of phosphinyl allenes is established for the first time. The palladium-catalyzed intramolecular cyclization provides an unprecedented cascade C?O cleavage and direct C?H alkenylation toward novel 3-alk
- Liu, Teng,Sun, Xue,Wu, Lei
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supporting information
p. 2005 - 2012
(2018/03/27)
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- Superoxide mediated isomerization of 4-aryl-but-1-ynes to 1-aryl-1,3-butadienes
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A new role of superoxide ion in the isomerization of homobenzylic acetylenes leading to 1-aryl-1,3-butadienes is reported. The unconventional reagent KO2 is found to be superior in performing this kind of isomerization over other the commonly u
- Khan, Faiz Ahmed,Budanur, Basavaraj M.
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p. 7600 - 7607
(2015/09/07)
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- Microwave-Assisted Organocatalyzed Rearrangement of Propargyl Vinyl Ethers to Salicylaldehyde Derivatives: An Experimental and Theoretical Study
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The microwave-assisted imidazole-catalyzed transformation of propargyl vinyl ethers (PVEs) into multisubstituted salicylaldehydes is described. The reaction is instrumentally simple, scalable, and tolerates a diverse degree of substitution at the propargylic position of the starting PVE. The generated salicylaldehyde motifs incorporate a broad range of topologies, spanning from simple aromatic monocycles to complex fused polycyclic systems. The reaction is highly regioselective and takes place under symmetry-breaking conditions. The preparative power of this reaction was demonstrated in the first total synthesis of morintrifolin B, a benzophenone metabolite isolated from the small tree Morinda citrifolia L. A DFT study of the reaction was performed with full agreement between calculated values and experimental results. The theoretically calculated values support a domino mechanism comprising a propargyl Claisen rearrangement, a [1,3]-H shift, a [1,7]-H shift (enolization), a 6π electrocyclization, and an aromatization reaction.
- Tejedor, David,Cotos, Leandro,Márquez-Arce, Daniel,Odriozola-Gimeno, Mikel,Torrent-Sucarrat, Miquel,Cossío, Fernando P.,García-Tellado, Fernando
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supporting information
p. 18280 - 18289
(2015/12/24)
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- A dynamic kinetic resolution of allyl alcohols by the combined use of lipases and [VO(OSiPh3)3]
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(Chemical Equation Presented) Mix and match: A new type of dynamic kinetic resolution of racemic allyl alcohols uses a combination of lipases and [VO(OSiPh3)3] (1). The 1,3-transposition of allyl alcohols catalyzed by 1 gave thermody
- Akai, Shuji,Tanimoto, Kouichi,Kanao, Yukiko,Egi, Masahiro,Yamamoto, Tomoko,Kita, Yasuyuki
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p. 2592 - 2595
(2007/10/03)
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