- Gram-scale synthesis of carboxylic acids via catalytic acceptorless dehydrogenative coupling of alcohols and hydroxides at an ultralow Ru loading
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Acceptorless dehydrogenative coupling (ADC) of alcohols and water/hydroxides is an emergent and graceful approach to produce carboxylic acids. Therefore, it is of high demand to develop active and practical catalysts/catalytic systems for this attractive transformation. Herein, we designed and fabricated a series of cyclometallated N-heterocyclic carbene-Ru (NHC-Ru) complexes via ligand tuning of [Ru-1], the superior complex in our previous work. Gratifyingly, gram-scale synthesis of carboxylic acids was efficiently enabled at an ultralow Ru loading (62.5 ppm) in open air. Moreover, effects of distinct ancillary NHC ligands and other parameters on this catalytic process were thoroughly studied, while further systematic studies were carried out to provide rationales for the activity trend of [Ru-1]-[Ru-7]. Finally, determination of quantitative green metrics illustrated that the present work exhibited superiority over representative literature reports. Hopefully, this study could provide valuable input for researchers who are engaging in metal-catalyzed ADC reactions.
- Chen, Cheng,Cheng, Hua,Verpoort, Francis,Wang, Zhi-Qin,Wu, Zhe,Yuan, Ye,Zheng, Zhong-Hui
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- Chemical tracer agent for fracturing as well as preparation method and application thereof
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The invention relates to a chemical tracer for fracturing and a preparation method and application thereof. The chemical tracer agent is fluoromethyl benzoic acid. The preparation method of the chemical tracer takes p-chlorofluoromethyl benzene as an initial raw material, and comprises a preparation step of a fluoromethyl benzene Grignard reagent, a preparation step of fluoromethyl benzoate and a preparation step of fluoromethyl benzoic acid. The invention further provides application of p-fluoromethyl benzoic acid as a chemical tracer in oil exploitation, trace detection can be realized, and the detection precision is improved.
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Paragraph 0063; 0069-0072; 0073-0074
(2021/05/29)
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- Substituted amide phenol compound and its preparation method, pharmaceutical composition and use thereof
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The invention discloses substituted-amide phenolic compounds, their preparation method, a pharmaceutical composition and an application thereof. The compounds have a structure as shown in the general formula I, wherein Z, L and Q are as defined in the spe
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- Accessing Difluoromethylated and Trifluoromethylated cis-Cycloalkanes and Saturated Heterocycles: Preferential Hydrogen Addition to the Substitution Sites for Dearomatization
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Reported here is a straightforward process in which a cyclic (alkyl)(amino)carbene/Rh catalyst system facilitates the preferential addition of hydrogen to the substitution sites of difluoromethylated and trifluoromethylated arenes and heteroarenes, leading to dearomative reduction. This strategy enables the diastereoselective synthesis of cis-difluoromethylated and cis-trifluoromethylated cycloalkanes and saturated heterocycles, and even allows formation of all-cis multi-trifluoromethylated cyclic products with a defined equatorial orientation of the di- and trifluoromethyl groups. Deuterium-labeling studies indicate that hydrogen preferentially attacks the substitution sites of planar arenes, resulting in dearomatization, possibly with heterogeneous Rh as the reactive species, followed by either reversible or irreversible hydrogen addition to the nonsubstitution sites.
- Zhang, Xue,Ling, Liang,Luo, Meiming,Zeng, Xiaoming
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supporting information
p. 16785 - 16789
(2019/11/11)
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- Transition-metal-free C-H oxidative activation: Persulfate-promoted selective benzylic mono- and difluorination
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An operationally simple and selective method for the direct conversion of benzylic C-H to C-F to obtain mono- and difluoromethylated arenes using Selectfluor as a fluorine source is developed. Persulfate can be used to selectively activate benzylic hydrogen atoms toward C-F bond formation without the aid of transition metal catalysts.
- Ma, Jing-Jing,Yi, Wen-Bin,Lu, Guo-Ping,Cai, Chun
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supporting information
p. 2890 - 2894
(2015/04/27)
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- NITROGENATED HETEROCYCLIC COMPOUND
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The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
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- COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES
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The invention provides novel tricyclic compounds of Formula (I) that inhibit β- secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
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Paragraph 00227
(2013/10/21)
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- Self-powered microscale pumps based on analyte-initiated depolymerization reactions
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Pump it up: Insoluble polymer films that depolymerize to release soluble monomeric products when exposed to a specific analyte act as a microscale pump. Products formed as a result of depolymerization amplify the signal and create a concentration gradient
- Zhang, Hua,Yeung, Kimy,Robbins, Jessica S.,Pavlick, Ryan A.,Wu, Meng,Liu, Ran,Sen, Ayusman,Phillips, Scott T.
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p. 2400 - 2404
(2012/04/23)
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- Novel Imidazole Derivatives Useful for the Treatment of Arthritis
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The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.
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- BICYCLIC COMPOUNDS USEFUL AS CATHEPSIN S INBHIBITORS
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Compounds of formula (I), wherein R1, R2, R3, Ra and E are are defined within, and pharmaceutically acceptable salts, solvates, hydrates and N-oxides thereof having utility in the treatment of disorders mediated by cathepsin S.
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- CATHEPSIN S INHIBITORS
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Compounds of the formula (I) where R1 is C1-C4 straight or branched alkyl, optionally substituted with up to three substituents selected from halo and hydroxy; R2 is halo, hydroxy, methyloxy, or C1-C2 alkyl, which alkyl is optionally substituted with up to three halogens or an hydroxy or a methyloxy; D is - C3-C7 alkylene-, thereby defining a cycloalkyl ring; E is -C(=O)-, -S(=O)m-, -NRdS(=O)m-, -NRaC(=O)-, -OC(=O)-, R3 is an optionally substituted carbocyclic or heterocyclic ring R10 is H, ORc, SRc or together with the gem H is =O or (ORc)2; Ra is independently selected from H, C1-C4 alkyl; have utility in the inhibition of cathepsin S and are thus useful pharmaceuticals against disorders such as autoimmune disorders and chronic pain.
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Page/Page column 96-97
(2010/11/08)
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- Fluorination process
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Aromatic compounds containing an α-fluoroalkyl or α,α-difluoroalkyl side chain are prepared by reacting selected aromatic compounds with a mixture of HF and a metal oxide which is PbO2 or NiO2 at -30° to +80° C. Exemplary is the conv
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