- BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
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It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
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Paragraph 0348; 0352; 0450; 0452
(2019/06/19)
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- Preparation and application of monodisperse polyethylene glycol monomethyl ether modified propofol prodrug
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Belonging to the field of organic chemistry and pharmaceutical chemicals, the invention discloses preparation and application of a monodisperse polyethylene glycol monomethyl ether modified propofol prodrug with a novel structure. Monodisperse polyethylene glycol monomethyl ether and propofol can be connected by an in-vivo degradable chemical bond to prepare a series of carbonic ester type and acetic ester type prodrugs respectively. By adjusting the length of the monodisperse polyethylene glycol monomethyl ether chain, the method can synthesize corresponding water-soluble propofol prodrugs, the longer the monodisperse polyethylene glycol monomethyl ether chain is, the better the water solubility is, along with the improvement of the water solubility, the prodrug can be made into aqueous solution preparations so as to avoid the defects of fat emulsion in propofol fat emulsions. The method provided by the invention has the advantages of simple reaction, mild conditions and low cost, andis convenient for industrial production.
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Paragraph 0042-0045
(2018/07/06)
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- Monodisperse oligoethylene glycols modified Propofol prodrugs
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The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.
- Deng, Tao,Mao, Xianglan,Li, Yu,Bo, Shaowei,Yang, Zhigang,Jiang, Zhong-Xing
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supporting information
p. 3502 - 3505
(2018/10/15)
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- A green and sustainable phosphine-free NHC-ruthenium catalyst for selective oxidation of alcohols to carboxylic acids in water
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In this work, we present a new catalytic system for the selective dehydrogenative oxidation of primary alcohols to carboxylic acids using a phosphine-free NHC-ruthenium catalyst in water under mild reaction conditions. With this catalytic system, a variety of primary alcohols have been converted to carboxylic acids respectively, in aqueous media, without using any additional oxidant; the only side product in this reaction is molecular hydrogen. This novel synthetic protocol is applied for direct oxidation of biologically active monosaccharides and polymers with primary alcohol groups in the side chain. The use of water as a solvent and oxygen donor as well as the absence of any toxic oxidizing agent make this atom economical reaction interesting from an environmental point of view.
- Malineni, Jagadeesh,Keul, Helmut,M?ller, Martin
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supporting information
p. 17409 - 17414
(2015/10/12)
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- Ceria supported gold-platinum catalysts for the selective oxidation of alkyl ethoxylates
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This work covers the development of a ceria based AuPt catalyst for the selective aerobic oxidation of alkyl ethoxylates to their corresponding carboxylic acids. By optimizing metal loading and the Au to Pt ratio the activity of the catalyst could be increased significantly, while maintaining total selectivity. Although the choice of ceria as a support helped to suppress intermediate metal leaching, the catalyst still showed poor long-term stability in repeated batches. The cause for deactivation could finally be identified by TPR studies as over-oxidation. These suspicions were confirmed by a long-term stability study in continuous-mode. It proved to be possible to deactivate the catalyst on purpose by employing unfavourable oxidising reaction conditions, i.e. low substrate concentrations and excess oxygen. By avoiding such unfavourable conditions either in continuous-flow mode or in repeated batches, the long-term stability of the catalyst increased tremendously. A substrate screening of various ethoxylates showed that the catalyst was very well-suited to selectively oxidize a wide range of alkyl ethoxylates.
- Heidkamp, Katharina,Aytemir, Memet,Vorlop, Klaus-Dieter,Pruesse, Ulf
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p. 2984 - 2992
(2013/11/06)
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- Chromium(VI) oxide oxidation of non-ethoxylated and ethoxylated alcohols for determination by electrospray ionization mass spectrometry
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A new derivatization procedure to increase the sensitivity of electrospray ionization mass spectrometry (ESI-MS) to non-ethoxylated and ethoxylated alcohols was investigated. The analytes were oxidized with chromium(VI) oxide and the resulting carboxylic and ethoxy-carboxylic acids were isolated by extraction with ethyl acetate; the extracts were alkalinized and infused into the ESI-MS system working in the negative-ion mode. The yields of the combined oxidation-extraction were ca. 100% for non-ethoxylated fatty alcohols dissolved in acetone and they decreased moderately in samples containing increasing amounts of water (e.g., a 75% yield was obtained with 50% water). Ethoxylated alcohols with more than two ethylene oxide units resulted in yields of ca. 60%. Low limits of detection (LODs) were obtained when the procedure was applied to the analysis of body- care products and cosmetics containing fatty alcohols, e.g., in a varicose-vein cream, the LODs were 25 μ cetyl alcohol and 7.5 μ stearyl alcohol (detected as palmitic acid and stearic acid, respectively) per gram of sample. High molecular mass alcohols were also detected in seawater after pre- concentration by solid-phase extraction. Thus, the proposed method is particularly valuable for use in industrial samples having complex matrices and in environmental samples and it is competitive with other methods for the analysis of trace amounts of fatty alcohols.
- Beneito-Cambra, Miriam,Bernabe-Zafon, Virginia,Simo-Alfonso, Ernesto F.,Ramis-Ramos, Guillermo
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experimental part
p. 2093 - 2100
(2011/11/06)
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- Homotropic cooperativity of cyclodextrin dimer as an artificial hydrolase
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Three kinds of cyclodextrin (CD) dimer (one homo-dimer of β-CD and two types of hetero-dimer of α-CD and β-CD) were synthesized as artificial hydrolases. The initial rates of the cleavage reaction of p-nitrophenyl methoxyethoxyethoxyacetate (8) by each of the three dimers were measured under the condition of excess of substrate at 25 °C in a pH 7.4 phosphate buffer solution. In a plot of initial rate against concentration of the substrate, the reaction with the homo-dimer (βCβH 5) gave a sigmoidal curve, whereas the reaction with either of the hetero-dimers gave a simple hyperbolic curve. Only βCβH 5 showed homotropic cooperativity, with a Hill constant of 1.8.
- Ikeda, Hiroshi,Nishikawa, Satoshi,Yamamoto, Yukinori,Ueno, Akihiko
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experimental part
p. 1 - 7
(2010/12/18)
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- Electroorganic synthesis in oil-in-water (O/W) nanoemulsion: TEMPO-mediated electrooxidation of amphiphilic alcohols in water
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Oil-in-water nanoemulsion which consisted of TEMPO, amphiphilic alcohols, and water offered unique reaction environments for electrooxidation of the alcohols to give the corresponding carboxylic acids in good to excellent yields.
- Kuroboshi, Manabu,Yoshida, Tomonori,Oshitani, Jun,Goto, Kuniaki,Tanaka, Hideo
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experimental part
p. 7177 - 7185
(2009/12/24)
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- Tempo-mediated oxidation of primary alcohols to carboxylic acids by exploitation of ethers inan aqueous-organicbiphase system
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Expeditious and benign methods for primary alcohol- carboxylicacid conversions with TEMPO were developed in abiphasic system composed of aslightlymiscible ether (THP) and aqueous layer. Easily available co-oxidants such as Py-HBr3, Bu4NBr3, and electrooxidation were successfully applied to generate N-oxoammonium species as a recyclable catalyst.
- Mei, Zhen-Wu,Ma, Li-Jian,Kawafuchi, Hiroyuki,Okihara, Takumi,Inokuchi, Tsutomu
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experimental part
p. 1000 - 1002
(2011/03/22)
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- Electroorganic synthesis in oil-in-water nanoemulsion: TEMPO-mediated electrooxidation of amphiphilic alcohols in water
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Oil-in-water nanoemulsions, consisting of TEMPO, amphiphilic alcohols, and water, offer unique reaction environments for electrooxidation of the alcohols to give the corresponding carboxylic acids in good to excellent yields. Georg Thieme Verlag Stuttgart.
- Yoshida, Tomonori,Kuroboshi, Manabu,Oshitani, Jun,Gotoh, Kuniaki,Tanaka, Hideo
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p. 2691 - 2694
(2008/02/12)
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- Synthesis and hydrolysis behavior of side-chain functionalized norbornenes
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The stabilities of various functionalized norbornenes that are monomers for the ring-opening metathesis polymerization (ROMP) in aqueous solution were evaluated toward hydrolysis under a range of temperatures (37, 60, and 80 °C) and pH values (3-9). All monomers contain hydrolyzable linkages to pendant functional groups, and conclusions were drawn relating to how the chemical diversity of these pendant functional groups, in accordance with the pH and temperature variations, affect hydrolysis of the aforementioned linkages. The hydrolysis was monitored by reverse phase HPLC analysis, and/or NMR spectroscopy. As expected, monomers containing ester linkages were fairly labile at higher pH values, while acetal-based linkers were cleaved at lower pH values. β-Amino ester groups experienced a significant increase in hydrolysis rate, while carboxylic acid-containing monomers did not follow any clear trend. Saccharide-containing monomers exhibited unique behaviors for various pH values and temperature ranges.
- Carlise, Joseph R.,Kriegel, Robert M.,Rees Jr., William S.,Weck, Marcus
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p. 5550 - 5560
(2007/10/03)
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- Permeable, water soluble, non-irritating prodrugs of chemotherapeutic agents with oxaalkanoic acids
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The present invention relates to the field of prodrugs of chemotherapeutic agents and method of use thereof.
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- CC-1065 analogs
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This invention provides some new synthetically obtained compounds of formula I and II STR1 which are useful as chemical intermediates. Representative formula I or II compounds have also been shown to possess useful ranges of antitumor activity in standard laboratory animal tests. In addition, the compounds of formula I or II can be linked to monoclonal antibodies, either directly or via known linking group, as a means of selectively delivering the CC-1065 analogs (Compounds of Formula I and II) to those target cells expressing the target antigen and thus selectively eliminating those diseased cells from the animal or human. Further, the compounds of formula I and II can be linked to soluble human CD4 or a soluble human CD4 protein fragment capable of binding to the gp120 envelope protein of the human immuno-virus and thus eliminate virally infected cells.
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- Hydrophilic Lipids
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The new triesters of glycerol 1-8 with different oligoethylene glycol carboxylic acids ("hydrophilic lipids") have been synthesized and their complexation with alkali and alkaline earth metal cations has been investigated.
- Heimann, Ulrich,Voegtle, Fritz
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p. 858 - 862
(2007/10/02)
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