- 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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- NMDA receptor antagonist and use thereof
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The present invention relates to an NMDA receptor antagonist and use thereof. The NMDA receptor antagonist is a compound as shown in the formula I, and pharmaceutically acceptable salts, enantiomers, diastereoisomers, tautomers, solvates, isotope substitutes, polymorphic substances, prodrugs or metabolites thereof, and in the formula, ring A, ring B and R2 are as described in the specification. The invention also provides pharmaceutical compositions containing the compounds, and applications of the compounds in preparation of drugs for treating or preventing NMDA receptor mediated diseases.
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Paragraph 0382-0386
(2021/08/11)
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- Aromatic compound, preparation method and use of aromatic compound
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The invention relates to an aromatic compound, a preparation method and use of the aromatic compound, andspecifically discloses a compound represented by the following formula (I), or a tautomer or anenantiomer or a diastereomer or a racemate of the compound or a mixture of the compound or a pharmaceutically acceptable salt of the compound. The invention further discloses a preparation method ofthe compound and application of the compound in treating nervous systemdiseases.
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- Enantioselective Protonation of Silyl Enol Ethers Catalyzed by a Chiral Pentacarboxycyclopentadiene-Based Bronsted Acid
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The enantioselective protonation of silyl enol ethers was realized in the presence of a pentacarboxycyclopenta-1,3-diene-based chiral Bronsted acid catalyst with water as an achiral proton source to give the corresponding α-aryl ketones in good yields and up to 75percent ee.
- An, Shaoyu,Li, Jun,Li, Pingfan,Yuan, Chao
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p. 1317 - 1320
(2019/06/19)
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- Ylide-Functionalized Phosphine (YPhos)-Palladium Catalysts: Selective Monoarylation of Alkyl Ketones with Aryl Chlorides
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Ylide-functionalized phosphine (YPhos) ligands allow the palladium-catalyzed α-arylation of alkyl ketones with aryl chlorides with record setting activity. Using a cyclohexyl-substituted YPhos ligand, a wide range of challenging ketone substrates was efficiently and selectively monoarylated under mild conditions. A newly designed YPhos ligand bearing tert-butyl groups on the coordinating phosphorus atom is already active at room temperature. The synthetic potential was demonstrated by gram-scale reactions and the succinct synthesis of ?-caprolactone derivatives.
- Hu, Xiao-Qiang,Lichte, Dominik,Rodstein, Ilja,Weber, Philip,Seitz, Ann-Katrin,Scherpf, Thorsten,Gessner, Viktoria H.,Goo?en, Lukas J.
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supporting information
p. 7558 - 7562
(2019/10/02)
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- Regioselective 1,2-Diol Rearrangement by Controlling the Loading of BF3·Et2O and Its Application to the Synthesis of Related Nor-Sesquiterene- and Sesquiterene-Type Marine Natural Products
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The regiocontrolled rearrangement of 1,2-diols has been achieved by controlling the loading of BF3·Et2O. Its applicability is showcased by the divergent synthesis of austrodoral, austrodoric acid, and 8-epi-11-nordriman-9-one, as well as a formal synthesis of siphonodictyal B and liphagal. A new light is shed on piancol-type rearrangements that will be useful in diversity-oriented synthesis of related natural products.
- Wang, Jun-Li,Li, Hui-Jing,Wang, Hong-Shuang,Wu, Yan-Chao
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p. 3811 - 3814
(2017/07/26)
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- Construction of a chiral quaternary carbon center by catalytic asymmetric alkylation of 2-arylcyclohexanones under phase-transfer conditions
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In this paper, we present an asymmetric alkylation of modified 2-arylcyclohexanones that employs a novel chiral ammonium bromide as a phase-transfer catalyst and an achiral auxiliary as a controller to improve the enantioselectivity to afford optically enriched products having a chiral quaternary carbon center.
- Kano, Taichi,Hayashi, Yumi,Maruoka, Keiji
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p. 7134 - 7137
(2013/06/27)
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- Arene CH-O hydrogen bonding: A stereocontrolling tool in palladium-catalyzed arylation and vinylation of ketones
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Weak is powerful: For the arylation of tin enolates, the palladium catalyst engages in weak CH-O hydrogen bonds to control stereoselectivity (see scheme). Similar catalysts capable of NH-O hydrogen bonding also works well. Copyright
- Huang, Zhiyan,Lim, Li Hui,Chen, Zuliang,Li, Yongxin,Zhou, Feng,Su, Haibin,Zhou, Jianrong
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supporting information
p. 4906 - 4911
(2013/06/05)
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- Copper(II)-catalyzed meta-selective direct arylation of α-aryl carbonyl compounds
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Strong competition: A method for the meta-selective arylation of the highly versatile α-aryl carbonyl motif using diaryliodonium salts is described. In this CuII-catalyzed process the remote carbonyl group is capable of overpowering even strongly para-directing functionalities to form the elusive meta-products (see scheme). Remarkably, the arylation process can also operate under metal-free conditions.
- Duong, Hung A.,Gilligan, Ruth E.,Cooke, Michael L.,Phipps, Robert J.,Gaunt, Matthew J.
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p. 463 - 466
(2011/03/16)
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- Chiral sulfinamide/achiral sulfonic acid cocatalyzed enantioselective protonation of enol silanes
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The application of chiral sulfinamides and achiral sulfonic acids as a cocatalyst system for enantioselective protonation reactions is described. Structurally simple, easily accessible sulfinamides were found to induce moderate-to-high ee's in the formation of 2-aryl-substituted cycloalkanones from the corresponding trimethylsilyl enol ethers.
- Beck, Elizabeth M.,Hyde, Alan M.,Jacobsen, Eric N.
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p. 4260 - 4263
(2011/10/08)
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- Carbene adduct of cyclopalladated ferrocenylimine catalyzed α-arylation of ketones with aryl chlorides or bromides
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Carbene adduct of cyclopalladated ferrocenylimine exhibited highly catalytic activity for the α-arylation of ketones with aryl halides. The corresponding products were obtained in moderate to excellent yields. Such protocol was applied to various ketones and a broad scope of aryl halides including aryl chlorides, bromides as well as unactivated and sterically hindered aryl halides.
- Zhang, Jinli,Yang, Xueqian,Cui, Xiuling,Wu, Yangjie
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experimental part
p. 8800 - 8807
(2011/12/02)
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- A boron-based synthesis of the natural product (+)-trans- dihydrolycoricidine
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Diastereoselective diboration results in the highly selective 1,4-dihydroxylation of chiral cyclohexadienes (see scheme). Together with the catalytic enantioselective conjugate allylboration, the diene diboration facilitates the asymmetric synthesis of the cytotoxic agent (+)-trans- dihydrolycoricidine (1). pin=pinacol. Copyright
- Poe, Sarah L.,Morken, James P.
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p. 4189 - 4192
(2011/06/20)
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- Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors
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Screening of the Roche compound library led to the identification of cis-N-(2-phenyl-cyclohexyl)-spiropiperidine 1 as structurally novel GlyT1 inhibitor. The SAR, which was developed in this series, resulted in the discovery of highly potent compounds displaying excellent selectivity against the GlyT2 isoform.
- Pinard, Emmanuel,Ceccarelli, Simona M.,Stalder, Henri,Alberati, Daniela
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p. 349 - 353
(2007/10/03)
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- Palladium-catalyzed regiocontrolled α-arylation of trimethylsilyl enol ethers with aryl halides
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(Diagram presented) Inter- and intramolecular arylations of trimethylsilyl enol ethers with aryl halides are accomplished regiospecifically in the presence of a palladium catalyst and tributyltin fluoride in refluxing benzene or toluene. The optimal catalyst system called for the use of Pd 2(dba)3 and tri-tert-butylphosphine in ca. 1:2 ratio. Aryl iodides, bromides, and chlorides are all effective arylation partners in this reaction.
- Iwama, Tetsuo,Rawal, Viresh H.
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p. 5725 - 5728
(2007/10/03)
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- TRIAZA-SPIROPIPERIDINE DERIVATIVES FOR USE AS GLYT-1 INHIBITORS IN THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
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The invention relates to compounds of the general formula (I), wherein A-A is -CH2-CH2-, -CH2-CH2-CH2-, -CH2-0- or -0-CH2-; x is hydrogen or hydroxy; R1 is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl; R2 is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl, or is lower alkyl, -(CH2)n--cycloalkyl, -(CH2)n-CF3, -(CH2)p-0-lower alkyl, -(CH2)1,2-phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy or trifluoromethyl, or is -(CH2)p-NRR", wherein W and R" form together with the N-atom a heterocyclic ring, selected from the group consisting of piperidine, morpholine, thiomorpholine or 1, I-dioxo thiomorpholine; R3, R4 are independently from each other hydrogen, lower alkyl, phenyl or benzyl; R5 is hydrogen, lower alkyl or benzyl; R6 is hydrogen or lower alkyl; n is 0, 1 or 2; and p is 2 or 3; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
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Page/Page column 34
(2010/02/11)
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- REACTIONS OF CONJUGATED ARYLAZOCYCLOALKENES WITH GRIGNARD REAGENTS-4. PARALLEL AND ANTIPARALLEL ATTACKS OF GRIGNARD HYDROCARBON MOIETY ON SOME ARYLAZOCYCLOALKENES
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Conjugated phenylazocycloalkenes sterically hindered towards the antiparallel attack react with PhMgBr via parallel attack, to give syn-phenylhydrazones.When such a sterical hindrance is absent in the azoalkenes, the reaction occurs via antiparallel attac
- Bozzini, Silvano,Gratton, Sergio,Lisini, Adriana,Pellizer, Giorgio,Risaliti, Amerigo
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p. 1459 - 1464
(2007/10/02)
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