242482-24-2Relevant academic research and scientific papers
Nickel-Catalyzed Desymmetrizing Cyclization of 1,6-Dienes to Construct Quaternary Stereocenters
Zhao, Tian-Yuan,Li, Ke,Yang, Liang-Liang,Zhu, Shou-Fei,Zhou, Qi-Lin
, p. 3814 - 3817 (2021)
A highly enantioselective and diastereoselective nickel-catalyzed desymmetrizing cyclization of 1,6-dienes was developed by using chiral spiro phosphoramidite ligands. The reaction provides a new atom- and step-economical approach to chiral spiro lactones and analogues bearing a quaternary stereocenter.
A Selective and Functional Group-Tolerant Ruthenium-Catalyzed Olefin Metathesis/Transfer Hydrogenation Tandem Sequence Using Formic Acid as Hydrogen Source
Zieliński, Grzegorz K.,Majtczak, Jaros?awa,Gutowski, Maciej,Grela, Karol
, p. 2542 - 2553 (2018/03/09)
A ruthenium-catalyzed transfer hydrogenation of olefins utilizing formic acid as a hydrogen donor is described. The application of commercially available alkylidene ruthenium complexes opens access to attractive C(sp3)-C(sp3) bond formation in an olefin metathesis/transfer hydrogenation sequence under tandem catalysis conditions. High chemoselectivity of the developed methodology provides a remarkable synthetic tool for the reduction of various functionalized alkenes under mild reaction conditions. The developed methodology is applied for the formal synthesis of the drugs pentoxyverine and bencyclane.
HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS
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Paragraph 00259, (2014/10/15)
Provided are certain histone deacetylase (HDAC) inhibitors of Formula (I), compositions thereof, and methods of their use.
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression
Wu, Yong-Jin,He, Huan,Bertekap, Robert,Westphal, Ryan,Lelas, Snjezana,Newton, Amy,Wallace, Tanya,Taber, Matthew,Davis, Carl,MacOr, John E.,Bronson, Joanne
, p. 2217 - 2228 (2013/05/08)
This report describes the synthesis, structure-activity relationships and activity of piperidine, homopiperidine, and azocane derivatives combining NK1 receptor (NK1R) antagonism and serotonin reuptake transporter (SERT) inhibition. Our studies culminated in the discovery of piperidine 2 and homopiperidine 8 as potent dual NK1R antagonists-SERT inhibitors. Compound 2 demonstrated significant activity in the gerbil forced swimming test, suggesting that dual NK1R antagonists-SERT inhibitors may be useful in treating depression disorders.
Nickel-catalyzed cyclization of α,ω-dienes: Formation vs. cleavage of C-C bonds
Necas, David,Tursky, Matyas,Tislerova, Iva,Kotora, Martin
, p. 671 - 674 (2007/10/03)
A combination of a catalytic amount of a Ni-phosphine complex and triethylaluminium or chlorodiethylaluminium is able to selectively cyclize a number of 1,7-heptadienes to methylidene(methyl)cyclopentanes and cyclopentenes even in cases where the dienes are prone to deallylation. the Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2006.
Cyclopentylamine and cyclohexylamine derivatives as NK-1/SSRI antagonists
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Page/Page column 8; 9, (2010/02/15)
The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.
Anti-infective agents
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Page/Page column 65-66, (2008/06/13)
Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.
ANTI-INFECTIVE AGENTS
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Page/Page column 127-128, (2010/02/11)
Compounds having the formula (I) are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.
Stereocontrol in sulfonyl radical-induced cyclizations of 1,6-dienes
Riggi, I. De,Nouguier, R.,Surzur, J. M.,Lesueur, C.,Bertrand, M.,et al.
, p. 229 - 235 (2007/10/02)
The radical addition of TsBr to 1,6-dienes leads to cyclopentane-based bromosulfones.These reactions proceed via the cyclization of substituted hex-5-enyl radicals.The control of the stereoselectivity depends on the number and nature of the substituents in position 3 with respect to the radical center.The products composition is well rationalized on the basis of stereoelectronic models.All the results are corroborated by theoretical force-field calculations.Key Words: sulfonyl radical / radical cyclization / MM2 calculations / stereoselectivity / substituted cyclopentane
