3132-64-7Relevant academic research and scientific papers
Visible-light assisted of nano Ni/g-C3N4 with efficient photocatalytic activity and stability for selective aerobic C?H activation and epoxidation
Akrami, Zahra,Hosseini-Sarvari, Mona
supporting information, (2020/10/13)
A selective, economical, and ecological protocol has been described for the oxidation of methyl arenes and their analogs to the corresponding carbonyl compounds and epoxidation reactions of alkenes with molecular oxygen (O2) or air as a green oxygen source, under mild reaction conditions. The nano Ni/g-C3N4 exhibited high photocatalytic activity, stability, and selectivity in the C?H activation of methyl arenes, methylene arenes, and epoxidation of various alkenes under visible- light irradiation without the use of an oxidizing agent and under base free conditions.
Synthesis, Characterization, and Application of Oxo-Molybdenum(V)-Corrolato Complexes in Epoxidation Reactions
Nayak, Manisha,Nayak, Panisha,Sahu, Kasturi,Kar, Sanjib
supporting information, p. 11654 - 11662 (2020/10/23)
Sharpless et al. have described, while performing the molybdenum-catalyzed epoxidation reaction of olefins using alkyl hydroperoxides, that the molybdenum-oxo moiety is an active catalytic species. Thus, continuous efforts have been made to synthesize molybdenum-oxo complexes of different ligand environments. While plenty of such works on molybdenum porphyrins are reported in the literature, related molybdenum corroles are very less reported. The synthesis and characterization of two new oxo-molybdenum(V)-corrolato complexes are described herein. Both the complexes have been fully characterized by several spectroscopic techniques in conjunction with single-crystal X-ray diffraction analysis. The efficacy of the oxo-molybdenum(V)-corrolato complexes for the catalytic epoxidation reaction of olefins with the help of hydroperoxides has also been explored. The catalytic application of oxo-molybdenum(V)-corrolato complexes in the epoxidation reaction has not been reported earlier. A mechanism has been proposed to explain the experimental findings.
Thiourea composite feed additive with urease inhibition activity and preparation method thereof
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Paragraph 0023-0037, (2019/04/29)
The invention discloses a thiourea composite feed additive with urease inhibition activity and a preparation method thereof, and belongs to the technical field of synthesis of feed additives. The technical scheme is characterized in that the compound structure of the thiourea composite feed additives is shown in the description. Compared with the prior art, the thiourea composite feed additive hasthe following beneficial effects: 1, the non-protein nitrogen group and the nitrogen-containing micromolecule urease inhibitor group can be linked together through the hydrophilic group by the feed additive obtained by the method, meanwhile, functions of supplementing non-protein nitrogen and inhibiting urease are provided; 2, the tandem non-protein nitrogen group and the nitrogen-containing small molecule urease inhibitor group are completed by 2-hydroxy propane through oxygen and imino, which is an excellent hydrophilic group, has good water solubility, has a stable molecular structure in vitro, and can effectively release a non-protein nitrogen group and a nitrogen-containing micromolecule urease inhibitor group in gastric juice; 3, the feed additive has no toxic or side effect; 4, themethod has simple operation and high product yield.
Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents
Xu, Yao,Chen, Shujun,Cao, Ying,Zhou, Pingzheng,Chen, Zhipeng,Cheng, Kui
, p. 253 - 266 (2018/05/29)
Toll-like receptor 4 (TLR4) initiates innate immune response to release inflammatory cytokines and has been pathologically linked to variety of inflammatory diseases. Recently, we found that Carvedilol, as the classic anti-heart failure and anti-inflammatory clinic drug, could inhibit the TLR4 signaling in the TLR4 overexpressed cells. Herein, we have designed and synthesized a small library of novel Carvedilol derivatives and investigated their potential inhibitory activity. The results indicate that the most potent compound 8a (SMU-XY3) could effectively inhibited TLR4 protein and the LPS triggered alkaline phosphatase signaling in HEK-Blue hTLR4 cells. It down regulated the nitric oxide (NO) in both RAW264.7 cells and BV-2 microglial cells, in addition to blocking the TNF-α signaling in ex-vivo human peripheral blood mononuclear cells (PBMC). More interestingly, 8a shows higher affinity to hyperpolarization-activated cyclic nucleotide-gated 4 (HCN4) over HCN2, which probably indicates the new application of TLR4 inhibitor 8a in heart failure, coronary heart disease, and other inflammatory diseases.
Synthetic method of tamoxifen medicine intermediate epibromohydrin
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Paragraph 0007; 0015; 0016, (2016/11/24)
A synthetic method of a tamoxifen medicine intermediate epibromohydrin includes the following steps: 1) adding 5.6 mol of 1-amino-3-bromo-propyl alcohol, 6.1-6.3 mol of a 2-bromophenol solution, 800 ml of a potassium bromide solution, 2.56 mol of aluminum oxide, 700 ml of hexane and 300 ml of a sodium sulfite solution into a reaction container provided with a distilling apparatus; 2) increasing the solution temperature to 70-75 DEG C and performing a reaction for 3-5 h, reducing the solution temperature to 50-55 DEG C, controlling the stirring rate to be 110-150 rpm, performing reflux for 90-110 min, and reducing the solution temperature to 10-13 DEG C, and allowing the solution to stand for 2-5 h to layer the solution; and 3) washing an oil layer successively with a salt solution, acetonitrile and isopropyl alcohol, performing pressure-reduced distillation and collecting the fraction at 80-85 DEG C, and performing re-crystallization in nitromethane to obtain the epibromohydrin crystal.
Manganese(II)/Picolinic Acid Catalyst System for Epoxidation of Olefins
Moretti, Ross A.,Du Bois,Stack, T. Daniel P.
supporting information, p. 2528 - 2531 (2016/07/06)
An in situ generated catalyst system based on Mn(CF3SO3)2, picolinic acid, and peracetic acid converts an extensive scope of olefins to their epoxides at 0 °C in 5 min, with remarkable oxidant efficiency and no evidence of radical behavior. Competition experiments indicate an electrophilic active oxidant, proposed to be a high-valent Mn = O species. Ligand exploration suggests a general ligand sphere motif contributes to effective oxidation. The method is underscored by its simplicity and use of inexpensive reagents to quickly access high value-added products.
METHOD FOR PURIFYING 2-FLUOROBUTANE
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Paragraph 0048, (2016/06/13)
The present invention is a method for 2-fluorobutane to obtain highly purified 2-fluorobutane through a process comprising a step for: bringing crude 2-fluorobutane that includes 5 to 50 wt % of butene into contact with a brominating agent that can form a bromonium ion in an aprotic polar solvent in the presence of water or an alcohol having up to 4 carbon atoms; converting the butene into compounds having a boiling point higher than that of 2-fluorobutane, then recovering 2-fluorbutane from the reaction solution; and purifying the recovered 2-fluorabutane by distillation.
Synthesis of ethyl (R)-4-cyano-3-hydroxybutyrate in high concentration using a novel halohydrin dehalogenase HHDH-PL from Parvibaculum lavamentivorans DS-1
Wan, Nan-Wei,Liu, Zhi-Qiang,Huang, Kai,Shen, Zhen-Yang,Xue, Feng,Zheng, Yu-Guo,Shen, Yin-Chu
, p. 64027 - 64031 (2015/02/19)
We identified and characterized a novel halohydrin dehalogenase HHDH-PL from Parvibaculum lavamentivorans DS-1. Study of substrate specificity indicated that HHDH-PL possessed a high activity toward ethyl (S)-4-chloro-3-hydroxybutanoate ((S)-CHBE). After optimizations of the pH and temperature, whole cell catalysis of HHDH-PL was applied to the synthesis of ethyl (R)-4-cyano-3-hydroxybutyrate (HN) at 200 g L-1 of (S)-CHBE, which gave 95% conversion and 85% yield in 14 h.
Biocatalytic and Structural Properties of a Highly Engineered Halohydrin Dehalogenase
Schallmey, Marcus,Floor, Robert J.,Hauer, Bernhard,Breuer, Michael,Jekel, Peter A.,Wijma, Hein J.,Dijkstra, Bauke W.,Janssen, Dick B.
, p. 870 - 881 (2013/07/25)
Two highly engineered halohydrin dehalogenase variants were characterized in terms of their performance in dehalogenation and epoxide cyanolysis reactions. Both enzyme variants outperformed the wild-type enzyme in the cyanolysis of ethyl (S)-3,4-epoxybutyrate, a conversion yielding ethyl (R)-4-cyano-3-hydroxybutyrate, an important chiral building block for statin synthesis. One of the enzyme variants, HheC2360, displayed catalytic rates for this cyanolysis reaction enhanced up to tenfold. Furthermore, the enantioselectivity of this variant was the opposite of that of the wild-type enzyme, both for dehalogenation and for cyanolysis reactions. The 37-fold mutant HheC2360 showed an increase in thermal stability of 8°C relative to the wild-type enzyme. Crystal structures of this enzyme were elucidated with chloride and ethyl (S)-3,4-epoxybutyrate or with ethyl (R)-4-cyano-3-hydroxybutyrate bound in the active site. The observed increase in temperature stability was explained in terms of a substantial increase in buried surface area relative to the wild-type HheC, together with enhanced interfacial interactions between the subunits that form the tetramer. The structures also revealed that the substrate binding pocket was modified both by substitutions and by backbone movements in loops surrounding the active site. The observed changes in the mutant structures are partly governed by coupled mutations, some of which are necessary to remove steric clashes or to allow backbone movements to occur. The importance of interactions between substitutions suggests that efficient directed evolution strategies should allow for compensating and synergistic mutations during library design.
USES OF FORMULATIONS OF THYROID HORMONE ANALOGS AND NANOPARTICULATE FORMS THEREOF TO INCREASE CHEMOSENSIVITY AND RADIOSENSITIVITY IN TUMOR OR CANCER CELLS
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, (2013/02/27)
Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.
