26915-75-3Relevant academic research and scientific papers
Synthesis and biological evaluation of a series of N-alkylated imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors
Kerscher-Hack, Silke,Renukappa-Gutke, Thejavathi,H?fner, Georg,Wanner, Klaus T.
, p. 852 - 880 (2016)
In this paper, we report the synthesis and biological evaluation of a series of 1,5- and 1,4- substituted derivatives of 1H-imidazol-4-ylacetic acid, a series of 1,2-substituted 3-(1H-imidazol-2-yl)propanoic acid and an N-substituted (2E)-3-(1H-imidazol-2-yl)prop-2-enoic acid as new mGAT3 inhibitors. The lipophilic moieties attached to the N-atom of the parent structures were delineated from the 2-[9-(4-methoxyphenyl)-9H-fluoren-9-yl]oxyethyl residue, known from a prototypic mGAT3 inhibitor. For the structure-activity-relationship studies, the spacer between the N-atom of the imidazole ring and the 2-[9-(4-methoxyphenyl)-9H-fluoren-9-yl] moiety was varied in length from three to six atoms, and in nature being either a pure saturated or unsaturated alkyl chain or an alkyl chain containing up to two ether functions. The compounds were characterized for inhibitory potencies at mouse GABA transporter proteins mGAT1–mGAT4. Among the 1,2-substituted compounds, the N-alkylated (2E)-3-(1H-imidazol-2-yl)prop-2-enoic acid 12e containing a C5O spacer exhibits a pIC50value of 5.13?±?0.04 at mGAT3, but is devoid of significant selectivity for this GABA transporter. However, the inhibitory potency displayed by 12e at mGAT3 nominally surpasses that of SNAP-5294 reported as the most potent inhibitor of mGAT3 so far.
Preparation method of ethylene sulfite
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Paragraph 0019, (2021/10/27)
The preparation method comprises the following steps 1) adding ethylene glycol disodium salt into a solvent, adding thionyl chloride dropwise to a certain temperature under the protection of nitrogen, adding the sodium bicarbonate aqueous solution to neutrality after a period of time, and separating the organic phase. 2) The organic phase was dried over anhydrous sodium sulfate, the solvent was recovered at atmospheric pressure, and vinyl sulfite was obtained under reduced pressure. 1) The synthetic method disclosed by the invention has the following beneficial effects that the ethylene glycol disodium salt is taken as a raw material and reacted with thionyl chloride in a solvent to synthesize ethylene sulfite. , The production cost is reduced, and great economic benefits and social benefits are achieved.
TEREPHTHALIC ACID ESTERS FORMATION
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Paragraph 0232, (2020/01/12)
The present disclosure relates to the formation of dimethyl terephthalate (DMT). The present invention also relates to the depolymerization of polyethylene terephthalate (PET) and the recovery of dimethyl terephthalate (DMT).
Synthesis of Functionalized 1,4-Dioxanes with an Additional (Hetero)Aliphatic Ring
Bondarenko, Andriy V.,Tolmachev, Andrey A.,Vashchenko, Bohdan V.,Grygorenko, Oleksandr O.
, p. 3696 - 3707 (2018/09/14)
An approach to the preparation of 2-mono-, 2,2- and 2,3-disubstituted 1,4-dioxane derivatives is described. The reaction sequence commences from readily available epoxides, in most cases prepared via the Corey-Chaikovsky reaction of the corresponding aldehydes and ketones. The key step of the method is epoxide ring opening with ethylene glycol monosodium salt, followed by further cyclization of the diols obtained. The utility of the approach was demonstrated by multigram preparation of novel functionalized 1,4-dioxanes bearing additional cycloalkane, piperidine or pyrrolidine rings, mostly spirocyclic compounds, which are advanced building blocks for medicinal chemistry.
Solubility of potassium and sodium orthophosphates in ethylene glycol
Kurzin,Evdokimov,Golikova,Fedorov
, p. 841 - 842 (2012/07/17)
Solubility of potassium and sodium orthophosphates in ethylene glycol was determined.
NOVEL HERBICIDES
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Page 43, (2008/06/13)
Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I are suitable for use as herbicides.
CHEMICAL COMPOUNDS
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Page 128, (2010/02/09)
Quinazoline derivatives of formula (I); for use in the treatment of proliferative diseases such as cancer and in the preparation of medicaments for use in the treatment of proliferative diseases, and to processes for their preparation, as well as pharmaceutical compositions containing them as active ingredient.
Process for producing a fluorine atom-containing sulfonyl fluoride compound
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Page/Page column 10-11, (2008/06/13)
The present invention provides a process whereby fluorine atom-containing sulfonyl fluoride compound(s) useful as e.g. materials for ion-exchange membranes, can be produced efficiently and at low cost without structural limitations while solving the difficulties in production. Namely, the present invention provides a process which comprises reacting XSO2RA-E1 (1) with RB-E2 (2) to form XSO2RA-E—RB (3), then reacting (3) with fluorine in a liquid phase to form FSO2RAF-EF-RBF (4), and further, decomposing the compound to obtain FSO2RAF-EF1 (5), wherein RA is a bivalent organic group, E1 is a monovalent reactive group, RB is a monovalent organic group, E2 is a monovalent reactive group which is reactive with E1, E is a bivalent connecting group formed by the reaction of E1 with E2, RAF is a bivalent organic group formed by the fluorination of RA, etc., RBF is the same group as RB, etc., EF is a bivalent connecting group formed by the fluorination of E, etc., EF1 is a monovalent group formed by the decomposition of EF, and X is a halogen atom.
Purified salt of beta-hydroxyethoxy acetic acid, purified 2-p-dioxanone, and manufacturing method therefor
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, (2008/06/13)
A purified salt of β-hydroxyethoxy acetic acid of formula (1) having a fusion peak-top temperature detected by differential scanning calorimetry (DSC) and a purified 2-p-dioxanone of formula (2) derived from the purified salt of β-hydroxyethoxy acetic acid of formula (1). (wherein in formula (1), n=1-2 , and if n=1, M is Na and/or K, and, if n=2, M is Ca and/or Mg.)
Stereochemical Studies on Hemiorthothiol and Hemiorthothiolate Tetrahedral Intermediates
Khouri, Farid F.,Kaloustian, Moses K.
, p. 6683 - 6695 (2007/10/02)
This study deals with hemiorthothiol-RC(OR')2SH-tetrahedral intermediates including (a) two acyclic ones of type , (b) two types of monocyclics and , and (c) four bicyclic systems , , , and .The breakdown of (R = Ph, R' = Et) led to thiono esters 34 and 35; that of (R = Me, Ph) resulted in hydroxy thiono esters 36-39, whereas the cleavage of (R =Me, Et) yielded thionolactones 49-53 and hydroxy thiono esters 55-58.The study of rigid bicyclic intermediates - helped uncover the role of stereoelectronic effects in the breakdown of hemiorthothiol tetrahedral intermediates.Finally, a family of isolable hemiorthothiolate tetrahedral intermediates-RC(OR')2S-+Na-viz. ->--> (monocyclic) and -> (bicyclic) is reported.
