936-44-7Relevant academic research and scientific papers
Construction of azacycles by intramolecular amination of organoboronates and organobis(boronates)
Xu, Peilin,Zhang, Mingkai,Ingoglia, Bryan,Allais, Christophe,Dechert-Schmitt, Anne-Marie R.,Singer, Robert A.,Morken, James P.
supporting information, p. 3379 - 3383 (2021/05/10)
Intramolecular amination of organoboronates occurs with a 1,2-metalate shift of an aminoboron ate complex to form azetidines, pyrrolidines, and piperidines. Bis(boronates) undergo site-selective amination to form boronate-containing azacycles. Enantiomerically enriched azacycles are formed with high stereospecificity.
The Titanium-Mediated Double Reductive Cleavage of Cyclic Sulfonamides for the Synthesis of Aryl Pyrrolidines
Khalifa, Aisha,Evans, Paul
, p. 2969 - 2975 (2019/02/26)
Reduction of a range of benzo-fused cyclic sulfonamides has been accomplished using low-valent titanium. This operationally simple method generates the corresponding aryl-substituted cyclic amines, typically, with good conversion. Notably, unlike our previous Li-NH3-based method, loss of heteroatom-based substituents (X) on the aromatic ring does not readily occur, and the robustness of this method was demonstrated with a synthesis of the Sceletium alkaloid mesembrane.
Synthesis of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazines that have antibacterial activity and also inhibit inorganic pyrophosphatase
Lv, Wei,Banerjee, Biplab,Molland, Katrina L.,Seleem, Mohamed N.,Ghafoor, Adil,Hamed, Maha I.,Wan, Baojie,Franzblau, Scott G.,Mesecar, Andrew D.,Cushman, Mark
, p. 406 - 418 (2014/01/17)
Inorganic pyrophosphatases are potential targets for the development of novel antibacterial agents. A pyrophosphatase-coupled high-throughput screening assay intended to detect o-succinyl benzoic acid coenzyme A (OSB CoA) synthetase inhibitors led to the unexpected discovery of a new series of novel inorganic pyrophosphatase inhibitors. Lead optimization studies resulted in a series of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazine derivatives that were prepared by an efficient synthetic pathway. One of the tetracyclic triazine analogues 22h displayed promising antibiotic activity against a wide variety of drug-resistant Staphylococcus aureus strains, as well as activity versus Mycobacterium tuberculosis and Bacillus anthracis, at a concentration that was not cytotoxic to mammalian cells.
SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1
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Paragraph 00417, (2014/07/08)
Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
Diastereoselective functionalisation of benzoannulated bicyclic sultams: Application for the synthesis of cis-2,4-diarylpyrrolidines
Kelleher, Susan,Quesne, Pierre-Yves,Evans, Paul
scheme or table, (2010/04/22)
The cis-dibromination of unsaturated bicyclic bridgehead sultams 5a and 5b, and experiments designed to understand the cisstereochemical outcome of these reactions, are described. In the case of 5b, a novel solvent dependent carbocation rearrangement occu
2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES AS TPK1 INHIBITORS
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Page/Page column 204; 205, (2008/06/13)
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof (I) wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
Double reduction of cyclic aromatic sulfonamides: A novel method for the synthesis of 2- and 3-aryl-substituted cyclic amines
Evans, Paul,McCabe, Thomas,Morgan, Ben S.,Reau, Sophie
, p. 43 - 46 (2007/10/03)
(Chemical Equation Presented) The facile double reduction of bicyclic aromatic sulfonamides was used to synthesize a variety of 2- and 3-aryl-substituted pyrrolidines and 2-phenylpiperidine. The method features a combined nitrogen protection and a traceless tether for the transposition of the aromatic moiety from nitrogen to carbon.
DIARYL ETHERS AS OPIOID RECEPTOR ANTAGONIST
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Page/Page column 195, (2008/06/13)
A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3', E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
N-Substituted-3-arylpyrrolidines: Potent and Selective Ligands at Serotonin 1A Receptor
Ahn, Kyo Han,Lee, Seok Jong,Lee, Chang-Ho,Hong, Chang Y.,Park, Tae Kyo
, p. 1379 - 1384 (2007/10/03)
3-Arylpyrrolidines are synthesized through the coupling of N-benzyl-3-(methanesulfonyloxy)pyrrolidine with diarylcuprates. Pharmacological evaluation of a series of N-substituted-3-arylpyrrolidines toward several neurotransmitter receptors indicated that some of them are good ligands for serotonin 1A receptor. Particularly, N-pyrrolidines were found to be potent and selective ligands. A preliminary biological evaluation for several selected compounds indicated that they are potentially effective antianxiety and antidepressant agents.
Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: Pharmacological evaluation for central dopaminergic and serotonergic activity
Sonesson, Clas,Wikstroem, Hakan,Smith, Martin W.,Svensson, Kjell,Carlsson, Arvid,Waters, Nicholas
, p. 241 - 246 (2007/10/03)
A series of 3-arylpyrrolidines has been synthesised via palladium catalyzed arylation and evaluated for dopaminergic and serotonergic activity in vitro and in vivo. Compounds substituted by electron withdrawing groups on the meta position of the aromatic ring, were found to be preferential dopamine autoreceptor antagonists.
