4137-81-9Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS DIHYDROOROTATE DEHYDROGENASE INHIBITORS
-
Page/Page column 90, (2021/08/14)
Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Embodiments of such compounds are represented by Formula (I) and Formula (II) as follows: and wherein R1, R2, R3, R4, R5, R6, R7, R8, X1, X2, X3, X4, Y and Z, are defined herein.
Nucleophilic reactivity of ethers against terminal epoxides in the presence of BF3: A mechanistic study
Kose, Aytekin,Altundas, Ramazan,Secen, Hasan,Kara, Yunus
, p. 1325 - 1330 (2013/08/23)
In the presence of BF3, a series of symmetrical and unsymmetrical ethers reacted with epichlorohydrin and 2-[(benzyloxy)methyl] oxirane, two terminal epoxides, to afford 1-alkoxy-3-chloropropan-2-ol and 1-alkoxy-3-(benzyloxy)propan-2-ol. The cleavage of unsymmetrical ethers occurred via an SN2 or SN1 mechanism. Secondary epoxides did not give similar ring-opening products. Copyright
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
-
Page/Page column 74, (2013/12/03)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.
NOVEL LIPASE INHIBITORS, REPORTER SUBSTRATES AND USES THEREOF
-
Paragraph 0159, (2014/01/07)
The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment o f disorders comprising administration o f novel diacylglycerol lipase inhibitors, and com -positions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods o f assaying enzymatic activity com -prising contacting a compound with a novel ether lipid reporter compound.
Enantioselective ring-opening reaction of epoxides with MeOH catalyzed by homochiral metal-organic framework
Tanaka, Koichi,Otani, Ken-Ichi,Murase, Takanori,Nishihote, Shyota,Urbanczyk-Lipkowska, Zofia
experimental part, p. 709 - 714 (2012/08/08)
Two new copper metal-organic frameworks containing 2,2′-dihydroxy-1, 1′-binaphthalene-5,5′-dicarboxylic acid (5,5′-H 2BDA) and 2,2′-dihydroxy-1,1′-binaphthalene-4,4′- dicarboxylic acid (4,4′-H2BDA) have been prepared. X-ray structure determination of [Cu2(5,5′-BDA)2(H 2O)2]·MeOH·2H2O (MOF-1) and [Cu2(4,4′-BDA)2(H2O)2] ·4H2O (MOF-2) revealed similar 2D sheet structures, containing square-grid coordination networks, but differences in the stacking motif. The desolvated MOF-1 and -2 were used as Lewis acid catalysts in the asymmetric ring-opening reaction of epoxides with MeOH.
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
-
Page/Page column 67, (2012/11/14)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula (I), wherein the variables are as defined herein.
Assay and inhibition of diacylglycerol lipase activity
Johnston, Meghan,Bhatt, Shachi R.,Sikka, Surina,Mercier, Richard W.,West, Jay M.,Makriyannis, Alexandros,Gatley, S. John,Duclos Jr., Richard I.
scheme or table, p. 4585 - 4592 (2012/08/08)
A series of N-formyl-α-amino acid esters of β-lactone derivatives structurally related to tetrahydrolipstatin (THL) and O-3841 were synthesized that inhibit human and murine diacylglycerol lipase (DAGL) activities. New ether lipid reporter compounds were developed for an in vitro assay to efficiently screen inhibitors of 1,2-diacyl-sn-glycerol hydrolysis and related lipase activities using fluorescence resonance energy transfer (FRET). A standardized thin layer chromatography (TLC) radioassay of diacylglycerol lipase activity utilizing the labeled endogenous substrate [1″- 14C]1-stearoyl-2-arachidonoyl-sn-glycerol with phosphorimaging detection was used to quantify inhibition by following formation of the initial product [1″-14C]2-arachidonoylglycerol and further hydrolysis under the assay conditions to [1-14C]arachidonic acid.
Ring-opening reactions of epoxides catalyzed by molybdenum(VI) dichloride dioxide
Jeyakumar, Kandasamy,Chand, Dillip Kumar
, p. 807 - 819 (2008/09/21)
Transformation of epoxides to β-alkoxy alcohols, acetonides, and α-alkoxy ketones is achieved by using molybdenum(VI) dichloride dioxide (MoO2Cl2) as a catalyst. Alcohol, aldehyde, oxime, tosyl, and tert-butyldimethylsilyl functional groups are tolerated during the methanolysis and acetonidation of the functionalized epoxides. No polymerization product is observed with any of the epoxides. Direct conversion of epoxides devoid of sensitive functional groups into the corresponding α-methoxy ketone is achieved in a single step by using the MoO2Cl 2/Oxone system. Georg Thieme Verlag Stuttgart.
Synthesis of 2,5-dihydrofurans via alkylidene carbene insertion reactions
Walker, Louise F.,Bourghida, Ahmed,Connolly, Stephen,Wills, Martin
, p. 965 - 981 (2007/10/03)
The insertion reaction of alkylidene carbenes is demonstrated to be an effective method for the synthesis of 2,5-dihydrofuran ring systems. The best results have been obtained on substrates containing electron-withdrawing substituents, which appear less prone to the competing rearrangement reaction. This insight has led to the development of a new method for the synthesis of the core structure of the squalestatin-zaragozic acid natural products.
Novel oxepane formation by TiCl4-catalyzed nucleophilic cleavage of 1- alkoxymethyl-6,8-dioxabicyclo[3.2.1]octanes
Fujiwara, Kenshu,Amano, Arika,Tokiwano, Tetsuo,Murai, Akio
, p. 1065 - 1080 (2007/10/03)
Introduction of an alkoxymethyl group at the C1 position in the 6,8- dioxabicyclo[3.2.1]octane system enabled novel formation of oxepane compounds in TiCl-4-catalyzed acetal cleavage reactions. (C) 2000 Elsevier Science Ltd.
