56703-34-5Relevant academic research and scientific papers
Photoinduced Hydrocarboxylation via Thiol-Catalyzed Delivery of Formate across Activated Alkenes
Alektiar, Sara N.,Wickens, Zachary K.
supporting information, p. 13022 - 13028 (2021/09/03)
Herein we disclose a new photochemical process to prepare carboxylic acids from formate salts and alkenes. This redox-neutral hydrocarboxylation proceeds in high yields across diverse functionalized alkene substrates with excellent regioselectivity. This operationally simple procedure can be readily scaled in batch at low photocatalyst loading (0.01% photocatalyst). Furthermore, this new reaction can leverage commercially available formate carbon isotologues to enable the direct synthesis of isotopically labeled carboxylic acids. Mechanistic studies support the working model involving a thiol-catalyzed radical chain process wherein the atoms from formate are delivered across the alkene substrate via CO2?- as a key reactive intermediate.
Synthesis method of succinic acid derivative or 3 -arylpropionic acid (by machine translation)
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Paragraph 0101-0114; 0115; 0141, (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)
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.
Direct β-Selective Hydrocarboxylation of Styrenes with CO2 Enabled by Continuous Flow Photoredox Catalysis
Seo, Hyowon,Liu, Aofei,Jamison, Timothy F.
, p. 13969 - 13972 (2017/10/17)
The direct β-selective hydrocarboxylation of styrenes under atmospheric pressure of CO2 has been developed using photoredox catalysis in continuous flow. The scope of this methodology was demonstrated with a range of functionalized terminal styrenes, as well as α-substituted and β-substituted styrenes.
SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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Page/Page column 46, (2013/10/22)
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
NOVEL THIOPHENE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE-1 RECEPTOR AGONISTS
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, (2011/10/01)
The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
Discovery of N-(3-fluorophenyl)-1-[(4-([(35)-3-methyl-1-piperazinyl]methyl) phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate
Westaway, Susan M.,Brown, Samantha L.,Fell, Stephen C. M.,Johnson, Christopher N.,MacPherson, David T.,Mitchell, Darren J.,Myatt, James W.,Stanway, Steven J.,Seal, Jon T.,Stemp, Geoffrey,Thompson, Mervyn,Lawless, Kirk,McKay, Fiona,Muir, Alison I.,Barford, Jonathan M.,Cluff, Chermaine,Mahmood, Sadhia R.,Matthews, Kim L.,Mohamed, Shiyam,Smith, Beverley,Stevens, Alexander J.,Bolton, Victoria J.,Jarvie, Emma M.,Sanger, Gareth J.
experimental part, p. 1180 - 1189 (2010/01/16)
N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl) acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the native rabbit motilin receptor where its agonist activity results in potentiation of the amplitude of neuronal-mediated contractions of isolated gastric antrum tissue. Compound 12 also possesses highly promising pharmacokinetic profiles in both rat and dog, and these results, in combination with further profiling in human native tissue and an in vivo model of gastrointestinal transit in the rabbit, have led to its selection as a candidate for further development.
HDAC INHIBITORS
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, (2008/06/13)
Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent =C- or =N-; W is a divalent radical -CH=CH- or CH2CH2-; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
Novel Thiophene Derivatives as Spingosine-1-Phosphate-1 Receptor Agonists
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Page/Page column 595, (2008/12/07)
The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
Peptide Synthesis. Part 1. Preparation and Use of Polar Supports based on Poly(dimethylacrylamide)
Arshady, Reza,Atherton, Eric,Clive, Derek L. J.,Sheppard, Robert C.
, p. 529 - 537 (2007/10/02)
Details are given of the preparation of two functionalised polar support materials based on poly(dimethylacrylamide).Their solvation and other properties make them particularly suitable for solid-phase synthesis of polar substances, particularly of peptides and oligonucleotides, and also for solid-phase peptide and protein sequencing.Procedures are described for solid-phase peptide synthesis and are illustrated by preparation of a decapeptide.
