- Rh-Catalyzed Annulation of Benzoic Acids, Formaldehyde, and Malonates via ortho-Hydroarylation to Indanones
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A three-component reaction from readily available low-cost materials of benzoic acids, formaldehyde, and malonates for the preparation of indanones by rhodium catalysis is reported. The annulation is initiated by an ortho-hydroarylation of benzoic acids, and a Lewis acid is not required. The solvent has a significant influence to the reaction, and 2-substituted or nonsubstituted indanones are obtained by the change of solvent.
- Yu, Shuling,Lv, Ningning,Hong, Chao,Liu, Zhanxiang,Zhang, Yuhong
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supporting information
p. 8354 - 8358
(2020/11/18)
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- Novel synthetic method for 7-halogen-1-indanone
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The invention discloses a novel synthetic method for 7-halogen-1-indanone. The reaction general formula of the method is shown in the description, wherein X is fluorine, chlorine or bromine. The method provided by the invention uses o-halogenated acetophenone as a starting raw material, an iron-catalyzed carbonyl methylenation reaction is performed to obtain a vinyl ketone, and acid-catalyzed ringclosure is performed to obtain the 7-halogen-1-indanone. The method provided by the invention has the advantages that the raw materials are simple and easy to obtain, the post-treatment is simple andthe total yield is high, and can provide an important reference for industrialized production.
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Paragraph 0035; 0036; 0037; 0038
(2018/07/07)
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- CARBAMATE DERIVATIVE COMPOUNDS, PROCESSES FOR PREPARING THEM AND THEIR USES
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The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a carbamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a carbamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
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Paragraph 223-225; 390-392
(2017/09/15)
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- SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
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Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
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Page/Page column 629
(2016/04/10)
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- NOVEL COMPOUND, AND KINESIN SPINDLE PROTEIN INHIBITOR AND APPLICATION THEREOF
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A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.
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Paragraph 0125
(2013/10/22)
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- COMPOUND, KINESIN SPINDLE PROTEIN INHIBITOR, AND APPLICATION THEREOF
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A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.
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Paragraph 0140
(2013/12/04)
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- SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
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Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
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Page/Page column 22; 23
(2008/12/04)
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- THERAPEUTIC FLUOROETHYLCYANO GUANIDINES
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Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
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Page/Page column 21
(2008/12/04)
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- A Convenient Synthesis of 7-Halo-1-indanones and 8-Halo-1-tetralones
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A regioselective oxidation of N-indan-4-yl-acetamide or N-(5,6,7,8-tetrahydronaphthalen-1-yl)acetamide with potassium permanganate followed by acidic hydrolysis gave 7-aminoindan-1-one or 8-aminotetral-1-one in good yield. The amino ketones were converted to the corresponding 7-haloindanone or the 8-halotetralone. Another method to prepare 7-haloindan-1-ones was completed by a cyclization of 3-chloro-1-(2-halophenyl)propan-1-one under Friedel-Crafts conditions to produce the product in gram quantity.
- Nguyen, Phong,Corpuz, Evelyn,Heidelbaugh, Todd M.,Chow, Ken,Garst, Michael E.
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p. 10195 - 10198
(2007/10/03)
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