35271-74-0Relevant articles and documents
Hydrogen-Bonding Catalyzed Ring-Closing C?O/C?O Metathesis of Aliphatic Ethers over Ionic Liquid under Metal-Free Conditions
Wang, Huan,Zhao, Yanfei,Zhang, Fengtao,Wu, Yunyan,Li, Ruipeng,Xiang, Junfeng,Wang, Zhenpeng,Han, Buxing,Liu, Zhimin
supporting information, p. 11850 - 11855 (2020/05/16)
O-heterocycles have wide applications, and their efficient and green synthesis is very interesting. Herein, we report hydrogen-bonding catalyzed ring-closing metathesis of aliphatic ethers to O-heterocycles over ionic liquid (IL) catalyst under metal- and solvent-free conditions. The IL 1-butylsulfonate-3-methylimidazolium trifluoromethanesulfonate ([SO3H-BMIm][OTf]) is discovered to show outstanding performance, better than the reported catalysts. An interface effect plays an important role in mediating the reaction rate due to the immiscibility between the products and the IL catalyst, and the products can be spontaneously separated. NMR analysis and DFT calculation suggest that a pair of cation and anion of [SO3H-BMIm][OTf] could form three strong H-bonds with an ether molecule, which catalyze the ether transformation via a cyclic oxonium intermediate. A series of O-heterocycles including tetrahydrofurans, tetrahydropyrans, morpholines and dioxane can be obtained from their corresponding ethers in excellent yields (e.g., >99 %). This work opens an efficient and metal-free way to produce O-heterocycles from aliphatic ethers.
Preparation method for refining high-purity 3-(4-chlorobenzene) glutaric acid
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Paragraph 0034-0081, (2019/01/14)
The invention discloses a preparation method for refining a high-purity 3-(4-chlorobenzene) glutaric acid. The preparation method comprises the steps of synthesizing a crude product of 3-(4-chlorobenzene) glutaric acid and purifying the crude product. An excellent technical effect is achieved and the contents of major impurity raw materials intermediate a and intermediate b as well as process impurities in the crude product of 3-(4-chlorobenzene) glutaric acid can be obviously reduced, in the manner of adopting a synthesis method for controlling the crude product of 3-(4-chlorobenzene) glutaric acid, purification processes from different documentaries and decontamination with methyl isobutyl ketone; the purity of 3-(4-chlorobenzene) glutaric acid detected with HPLC can reach up to above 99.8%; the limits of impurities are all less than 0.1%.
CHEMICAL COMPOUNDS AS ATF4 PATHWAY INHIBITORS
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Page/Page column 179; 180, (2019/01/06)
The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula (IIIQ): wherein X6', a, b, C8', D8', L82', L83', R81', R82', R83', R84', R85', R86', z82', z84', z85', and z86' are as defined herein; or salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
A balufen green industrial production method (by machine translation)
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Paragraph 0023; 0028, (2017/05/02)
The invention discloses a balufen green preparation method, which belongs to the technical field of drug synthesis. The method to the chlorobenzene as a starting material, by Knoevenagel condensation, alkali hydrolysis, sub-amide, alkali hydrolysis and Hofmann degradation 5 step reaction make the consistent with the clinical pharmaceutical balufen. Raw materials of this invention extremely easy, low cost, simple synthesis operation, are basically all aqueous reaction under the condition of, environmental pollution is very small, high yield, is a brand new industrial production balufen method. (by machine translation)
Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors
Yang, Liuqing,Liu, Wei,Mei, Hanbing,Zhang, Yuan,Yu, Xiaojuan,Xu, Yufang,Li, Honglin,Huang, Jin,Zhao, Zhenjiang
, p. 671 - 676 (2015/04/27)
Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs. This journal is
Three multicomponent reactions of 3,5-dimethyl-4-nitroisoxazole
Adamo, Mauro F.A.,Konda, Vivekananda R.,Donati, Donato,Sarti-Fantoni, Piero,Torroba, Tomas
, p. 9741 - 9745 (2008/02/12)
The title compound is used to prepare 3-arylglutaric acids, bis-isoxazoles and bis-pyrazoles from commercially available materials. The methodologies described have afforded important synthetic intermediates in high yields and without the use of chromatography.
Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
Wendt, John A.,Wu, Hongwei,Stenmark, Heather G.,Boys, Mark L.,Downs, Victoria L.,Penning, Thomas D.,Chen, Barbara B.,Wang, Yaping,Duffin, Tiffany,Finn, Mary Beth,Keene, Jeffery L.,Engleman, V. Wayne,Freeman, Sandra K.,Hanneke, Melanie L.,Shannon, Kristen E.,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marissa,Klover, Jon A.,Westlin, William,Nickols, G. Allen,Russell, Mark A.
, p. 845 - 849 (2007/10/03)
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ 3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
Enzymatic desymmetrization of 3-arylglutaric acid anhydrides
Fryszkowska, Anna,Komar, Marta,Koszelewski, Dominik,Ostaszewski, Ryszard
, p. 2475 - 2485 (2007/10/03)
Optically active (R)- and (S)-3-arylglutaric acid monoesters 3 were synthesized in quantitative yields and good stereoselectivities by lipase-catalyzed desymmetrization of the corresponding 3-arylglutaric anhydrides 2 with alcohols. It was observed that the stereochemical outcome of the reaction was influenced by the substituents present on the aromatic ring. The influence of the enzyme, alcohol, and solvent was systematically examined. Absolute configurations of the monoesters 3 were assigned by chemical correlation to corresponding lactones 4.
Solid-phase synthesis of a nonpeptide RGD mimetic library: New selective αvβ3 integrin antagonists
Sulyok,Gibson,Goodman,H?lzemann,Wiesner,Kessler
, p. 1938 - 1950 (2007/10/03)
The solid-phase synthesis of a low molecular weight RGD mimetic library is described. Activities of the compounds in inhibiting the interaction of ligands, vitronectin and fibrinogen, with isolated immobilized integrins αvβ3 and αIIbβ3 were determined in a screening assay. Highly active and selective nonpeptide αvβ3 integrin antagonists with regard to orally bioavailability were developed, based on the aza-glycine containing lead compound 1. An important variation is the substitution of the aspartic amide of 1 by an aromatic residue. Furthermore, different guanidine mimetics have been incorporated to improve the pharmacokinetic profile. Exchange of the β-amino acid NH by a methylene moiety in one set of RGD mimetics leads to the azacarba analogue compounds representing a novel peptidomimetic approach, which should increase the metabolic stability.
