458-45-7Relevant articles and documents
Synthesis method of succinic acid derivative or 3 -arylpropionic acid (by machine translation)
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Paragraph 0101-0114; 0115; 0131, (2020/10/30)
The invention discloses a synthesis method of a succinic acid derivative or 3 -arylpropionic acid, which comprises the following steps: adding a base in a drying reaction tube and CO removing CO. 2 The reaction is carried out under the irradiation of visible light, the reaction is carried out under visible light irradiation, and then separation and purification are carried out to obtain the butanedioic acid derivative or 3 -arylpropionic acid product; the base comprises sodium tert-butoxide, potassium tert-butoxide, lithium tert-butyl alcohol and 4 - potassium carbonate; and the reaction substrate comprises an acrylate compound or an aryl vinyl compound. CO can be induced by visible light. 2 The scheme provided by the invention is mild in reaction condition and wide in reaction 3 - substrate selectivity, and the reaction substrate is wide in selectivity, the raw materials are cheap and easily available, and the method has a good industrial application prospect. (by machine translation)
Generalized Chemoselective Transfer Hydrogenation/Hydrodeuteration
Wang, Yong,Cao, Xinyi,Zhao, Leyao,Pi, Chao,Ji, Jingfei,Cui, Xiuling,Wu, Yangjie
supporting information, p. 4119 - 4129 (2020/08/10)
A generalized, simple and efficient transfer hydrogenation of unsaturated bonds has been developed using HBPin and various proton reagents as hydrogen sources. The substrates, including alkenes, alkynes, aromatic heterocycles, aldehydes, ketones, imines, azo, nitro, epoxy and nitrile compounds, are all applied to this catalytic system. Various groups, which cannot survive under the Pd/C/H2 combination, are tolerated. The activity of the reactants was studied and the trends are as follows: styrene'diphenylmethanimine'benzaldehyde'azobenzene'nitrobenzene'quinoline'acetophenone'benzonitrile. Substrates bearing two or more different unsaturated bonds were also investigated and transfer hydrogenation occurred with excellent chemoselectivity. Nano-palladium catalyst in situ generated from Pd(OAc)2 and HBPin extremely improved the TH efficiency. Furthermore, chemoselective anti-Markovnikov hydrodeuteration of terminal aromatic olefins was achieved using D2O and HBPin via in situ HD generation and discrimination. (Figure presented.).
Method for selective reduction α, β - unsaturated carbonyl compound carbon-carbon double bond (by machine translation)
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Paragraph 0047-0050, (2020/06/17)
The invention discloses a method for selectively reducing carbon-carbon double bonds in α and β - unsaturated carbonyl compounds, which comprises the following steps of adding α, β - unsaturated carbonyl compounds shown in formula (I) in an electrolysis system and reducing α and β - unsaturated carbonyl compounds with carbonyl-conjugated carbon-carbon double bonds through an electrochemical cathodic reduction reaction. Compared with the reported method, the method disclosed by the invention does not use a metal catalyst and an external oxidant; and the reaction raw material and the electrolyte are low in price, nontoxic and tasteless, simple and convenient in post-treatment. (by machine translation)
Reactivity control of a photocatalytic system by changing the light intensity
Kerzig, Christoph,Wenger, Oliver S.
, p. 11023 - 11029 (2019/12/28)
We report a novel light-intensity dependent reactivity approach allowing us to selectively switch between triplet energy transfer and electron transfer reactions, or to regulate the redox potential available for challenging reductions. Simply by adjusting the light power density with an inexpensive lens while keeping all other parameters constant, we achieved control over one- and two-photon mechanisms, and successfully exploited our approach for lab-scale photoreactions using three substrate classes with excellent selectivities and good product yields. Specifically, our proof-of-concept study demonstrates that the irradiation intensity can be used to control (i) the available photoredox reactivity for reductive dehalogenations to selectively target either bromo- or chloro-substituted arenes, (ii) the photochemical cis-trans isomerization of olefins versus their photoreduction, and (iii) the competition between hydrogen atom abstraction and radical dimerization processes.
Ligand-Controlled Regioselective Hydrocarboxylation of Styrenes with CO2 by Combining Visible Light and Nickel Catalysis
Meng, Qing-Yuan,Wang, Shun,Huff, Gregory S.,Konig, Burkhard
supporting information, p. 3198 - 3201 (2018/03/13)
The ligand-controlled Markovnikov and anti-Markovnikov hydrocarboxylation of styrenes with atmospheric pressure of CO2 at room temperature using dual visible-light-nickel catalysis has been developed. In the presence of neocuproine as ligand, the Markovnikov product is obtained exclusively, while employing 1,4-bis(diphenylphosphino)butane (dppb) as the ligand favors the formation of the anti-Markovnikov product. A range of functional groups and electron-poor, -neutral, as well as electron-rich styrene derivatives are tolerated by the reaction, providing the desired products in moderate to good yields. Preliminary mechanistic investigations indicate the generation of a nickel hydride (H-NiII) intermediate, which subsequently adds irreversibly to styrenes.
A Ligand-Directed Catalytic Regioselective Hydrocarboxylation of Aryl Olefins with Pd and Formic Acid
Liu, Wei,Ren, Wenlong,Li, Jingfu,Shi, Yuan,Chang, Wenju,Shi, Yian
supporting information, p. 1748 - 1751 (2017/04/11)
An effective Pd-catalyzed hydrocarboxylation of aryl olefins with Ac2O and formic acid is described. A variety of 2- and 3-arylpropanoic acids can be regioselectively formed by the judicious choice of ligand without the use of toxic CO gas.
NOVEL INHIBITORS
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Page/Page column 91; 177, (2014/09/29)
The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N- terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
17a-HYDROXYLASE/C17,20-LYASE INHIBITORS
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Paragraph 1108, (2014/03/21)
The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
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Page/Page column 181, (2012/04/04)
The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
PREPARATION OF FIPAMEZOLE
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Page/Page column 14; 15, (2011/02/24)
The application relates to processes for preparing fipamezole and its pharmaceutically acceptable salts, and intermediates thereof. It also provides intermediate compounds of Formula III and Formula IV, and processes for their preparation.
