107-29-9Relevant articles and documents
Lewis acidic strength controlled highly selective synthesis of oxime via liquid-phase ammoximation over titanosilicates
Zhuo, Zuoxi,Wu, Lizhi,Wang, Lei,Ding, Yichun,Zhang, Xiaoqian,Liu, Yueming,He, Mingyuan
, p. 55685 - 55688 (2014)
The Lewis acidity of titanosilicates determines the selectivity of the oxime in ammoximation. Higher Lewis acidic strength of Ti active sites could promote free H2O2 to participate in the highly efficient formation of NH2OH by lowering the reaction activation energy for the formation of Ti-OOH species, and thus fundamentally suppress the side reactions of deep oxidation.
Access to multi-functionalized oxazolines via silver-catalyzed heteroannulation of enamides with sulfoxonium ylides
Liu, Rui-Hua,Shan, Qi-Chao,Gao, Ya,Loh, Teck-Peng,Hu, Xu-Hong
, p. 1411 - 1414 (2021)
Disclosed herein is an efficient Ag-catalyzed [4 + 1] heteroannulation reaction of enamides with α-carbonyl sulfoxonium ylides. The diastereoselective transformation provides a practical access to a diverse range of multi-functionalized oxazoline derivatives. The synthetic utility of the resultant tetra-substituted oxazolines is further demonstrated by a series of useful manipulations into valuable building blocks of pharmaceutical relevance.
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator
Aicher, Thomas D.,Baer, Brian R.,Boyd, Steven A.,Chicarelli, Mark D.,Condroski, Kevin R.,DeWolf, Walter E.,Fischer, John,Frank, Michele,Hingorani, Gary P.,Hinklin, Ronald J.,Lee, Patrice A.,Neitzel, Nickolas A.,Pratt, Scott A.,Singh, Ajay,Sullivan, Francis X.,Turner, Timothy,Voegtli, Walter C.,Wallace, Eli M.,Williams, Lance
, (2019/12/24)
Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is also responsible for reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to have an inadequacy or defect in one or both of these processes, identifying compounds that can activate GK could provide a therapeutic benefit. Herein we report the further structure activity studies of a novel series of glucokinase activators (GKA). These studies led to the identification of pyridine 72 as a potent GKA that lowered post-prandial glucose in normal C57BL/6J mice, and after 14d dosing in ob/ob mice.
Separation and purification method for acetaldehyde oxime
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Paragraph 0031-0065, (2020/02/19)
The invention discloses a separation and purification method for acetaldehyde oxime, and relates to the technical field of separation and purification of oxime. The method comprises the following steps: 1) performing an oxime exchange reaction on cyclohexanone oxime and acetaldehyde to obtain an acetaldehyde oxime reaction solution, performing neutralization by using a base, and after the neutralization is completed, controlling the pH of the acetaldehyde oxime reaction solution to 7; 2) adding toluene into the acetaldehyde oxime reaction solution, performing distillation under reduced pressure to separate acetaldehyde oxime and cyclohexanone to obtain an acetaldehyde oxime and toluene mixed liquid and the cyclohexanone; 3) adding extractant water into the obtained acetaldehyde oxime and toluene mixed liquid, and separating the toluene and the acetaldehyde oxime by using a continuous extraction process to obtain an acetaldehyde oxime aqueous solution and the toluene, respectively; and4) performing reduced-pressure rectification on the acetaldehyde oxime aqueous solution to obtain the acetaldehyde oxime product. The method provided by the invention has simple operation and high purity and yield of the acetaldehyde oxime, does not generate waste liquid, and is an environment-friendly green process route for production separation and purification of the acetaldehyde oxime.
A preparation method of acetaldoxime
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Paragraph 0017-0036, (2019/03/24)
The present invention relates to organic chemical synthesis technology field, in particular to a acetaldoxime preparation method. The invention acetaldoxime preparation method, comprises the following steps: 1) the hydroxylamine and distilled water and stirring to dissolve, then dropping in the ice water bath under the conditions of the acetaldehyde, acetic acid catalyst, after the completion of the dropping 0 - 10 °C stirring reaction for 10 - 30 minutes, make acetaldoxime solution; 2) in the step 1) in dichloromethane is used for extraction of acetaldoxime solution, extraction solution after drying with anhydrous sodium sulfate, the solvent first atmospheric distillation, distillation under reduced pressure, collecting the fraction, transparent liquid is acetaldoxime. The invention acetaldoxime preparation method to acetic acid as catalyst, hydroxylamine and acetaldehyde as raw material to make the acetaldoxime solution, after extraction, drying, atmospheric fractionation, distilling and getting the colorless transparent liquid is acetaldoxime, acetaldoxime made without water, purity ≥ 99%, yield ≥ 92%.
Method for preparing oxime
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Paragraph 0034; 0035; 0036, (2018/09/08)
The invention discloses a method for preparing oxime. The method is characterized in that catalytic reaction for oxime synthesis is performed by using a titanium silicate molecular sieve of a MSE topological structure as a catalyst and using ketone or aldehyde, ammonia and hydrogen peroxide as a reaction system, wherein in the reaction system, the weight ratio of ketone or aldehyde to the catalystto a solvent is 1:(0.03 to 0.15):(1 to 15); the molar ratio of the ketone or aldehyde to the ammonia is 1:(1 to 4); the catalyst is Ti-MSE or a combination body of Ti-MSE and silicon dioxide or a titanium-containing molecular sieve. Compared with the prior art, the method has the advantages that the selectivity is high; the catalytic activity is high; the aftertreatment is simple and convenient;the conversion rate of reactants of ketone or aldehyde reaches up to 99 percent; the product oxime selectivity reaches up to 99 percent, so that the molecular sieve shows excellent catalytic activityin the specific catalysis field; the application field of the molecular sieve is expanded; a novel and environment-friendly ammoxidation oxime preparation path is provided; certain industrial popularization and application prospects and prominent economic values are realized.
Chemically synthesized heterocyclic insecticide intermediate and preparation method thereof
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Paragraph 0042, (2017/11/29)
The invention discloses a chemically synthesized heterocyclic insecticide intermediate and a preparation method thereof. The chemically synthesized heterocyclic insecticide intermediate is prepared from the following raw materials in parts by weight: 100 to 150 parts of distilled water, 65 to 90 parts of hydroxylamine sulphate, 80 to 100 parts of ammonia water, 20 to 30 parts of acetaldehyde, 30 to 40 parts of sodium hydroxide, 35 to 50 parts of potassium permanganate, 45 to 60 parts of concentrated hydrochloric acid and 15 to 20 parts of saturated salt water. According to the chemically synthesized heterocyclic insecticide intermediate, the preparation method is relatively mature and a technology is relatively simple; a production progress, and the dosage ratio of each index are convenient to control and the raw materials for synthesizing are materials which are common in the market and are cheap and easy to obtain; the yield of the prepared intermediate methylthioacetaldoxime reaches 75 percent to 80 percent and is much higher than the average yield of an existing market; the medicinal effect is improved; the intermediate methylthioacetaldoxime has stable chemical properties and does not have viscous decomposition or deterioration problems and the like at room temperature, and the economic benefits are improved.
An efficient protocol for the synthesis of six-membered N, O-heterocycles via a 1,3-dipolar (3+3) cycloaddition between nitrile oxide and α-diazo esters
Kuruba, Bharath Kumar,Vasanthkumar, Samuel
, p. 3860 - 3865 (2017/06/14)
In this manuscript, we are reporting an efficient protocol for the construction of highly functionalized N, O-heterocyclic derivatives such as 1,2,4-oxadiazine and 1,4,2-dioxazine-6-carboxylate derivatives via a 1,3-dipolar (3 + 3) cycloaddition between nitrile oxide and unprotected α-diazo esters in the presence of 2 mol% Cu(OTf)2 catalyst. The expected N, O-heterocycles were obtained in excellent yields. These N, O-heterocycles are known to exhibit insecticidal and acaricidal properties.
Investigations of the Thermal Responsiveness of 1,4,2-Oxathiazoles
Hewitt, Russell J.,Ong, Michelle Jui Hsien,Lim, Yi Wee,Burkett, Brendan A.
, p. 6687 - 6700 (2015/10/29)
The first systematic study of the thermal rearrangement/fragmentation of 5,5-disubstituted 1,4,2-oxathiazoles into isothiocyanates is reported. Structure-activity relationships reveal that the choice of substituent at the 5-position of the 1,4,2-oxathiazoles is the predominant factor to influence the ease of fragmentation.
Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists
Soni, Ajay,Rehman, Abdul,Naik, Keshav,Dastidar, Sunanda,Alam,Ray, Abhijit,Chaira, Tridib,Shah, Vanya,Palle, Venkata P.,Cliffe, Ian A.,Sattigeri, Viswajanani J.
, p. 1482 - 1485 (2013/03/14)
A novel set of compounds containing a 4,5-dihydro-5-methylisoxazoline have been successfully designed as VLA-4 receptor antagonists. Compound (14p) had a high receptor binding affinity of 4 nM and also found to be metabolically stable in vitro.
