- Bromination of α-Diazo Phenylacetate Derivatives Using Cobalt(II) Bromide
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A method for the bromination of α-diazo phenylacetate derivatives using cobalt(II) bromide is described. This bromination reaction features a short reaction time, broad substrate scope, operational simplicity, acid-free conditions, and gram-scalability. (Figure presented.).
- Wang, Haifeng,Sun, Xiangli,Hu, Manman,Zhang, Xiaoyi,Xie, Lele,Gu, Shuangxi
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supporting information
p. 3347 - 3351
(2020/07/04)
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- Pd-catalyzed divergent C(sp2)-H Activation/Cycloimidoylation of 2-Isocyano-2,3-diarylpropanoates
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A Pd-catalyzed site-selective C(sp2)-H activation/cycloimidoylation of 2-isocyano-2,3-diarylpropanoates to construct diverse cyclic imine products has been developed. Six-membered 3,4-dihydroisoquinolines containing a C3 quaternary carbon cente
- Tang, Shi,Yang, Sheng-Wen,Sun, Hongwei,Zhou, Yali,Li, Juan,Zhu, Qiang
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supporting information
p. 1832 - 1836
(2018/04/14)
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- Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modeling
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The design, synthesis, and antiplasmodial activity of antimalarial heterodimers based on the 1,4-bis(3-aminopropyl)piperazine linker is reported. In this series key structural elements derived from quinoline antimalarials were coupled to fragments capable
- Gemma, Sandra,Kukreja, Gagan,Campiani, Giuseppe,Butini, Stefania,Bernetti, Matteo,Joshi, Bhupendra P.,Savini, Luisa,Basilico, Nicoletta,Taramelli, Donatella,Yardley, Vanessa,Bertamino, Alessia,Novellino, Ettore,Persico, Marco,Catalanotti, Bruno,Fattorusso, Caterina
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p. 3535 - 3539
(2008/02/07)
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- Method of treating depression using azabicyclohexanes
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The present invention concerns certain novel substituted 3-azabicyclo[3.1.0]hexanes and a method of treating depression and stress in a warm-blooded animal, comprising the administration of substituted 3-azabicyclo[3.1.0]hexanes.
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- 1-Aryl-3-azabicyclohexanes, a New Series of Nonnarcotic Analgesic Agents
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A series of 1-aryl-3-azabicyclohexanes was synthesized by hydride reduction of 1-arylcyclopropanedicarboximides.Hydroxyphenyl analogues 20, 22, and 24 were prepared by EtSNa-DMF ether cleavage of the corresponding methoxyphenyl analogues 2m, 2n, and 23, respectively, with the secondary amines 20 and 22 going through the N-formyl intermediates 19 and 21.The p-ethoxy analogue 26 was obtained by O-ethylation of 19, followed by base hydrolysis of the amide 25.The greatest analgesic potency in mouse writhing and rat paw-pain assays was observed for para-substituted compounds.Bicifadine, 1-(4-methylphenyl)-3-azabicyclohexane (2b), was the most potent member of the series and is presently undergoing clinical trials in man.Analgesic activity of 2b is limited to the (+) enantiomer 2v, which has the 1R,5S absolute configuration as determined by single-crystal X-ray analysis.The N-methyl analogue (27d) of 2b showed significant analgesic potency, whereas the N-allyl (27a), N-(cyclopropylmethyl) (27b), and N-(n-hexyl) (27c) analogues were inactive.Bicifadine (2b) showed a nonnarcotic profile different from analogous azabicycloalkane and 3-phenylpyrrolidine analgesics.
- Epstein, Joseph W.,Brabander, Herbert J.,Fanshawe, William J.,Hofmann, Corris M.,McKenzie, Thomas C.,et al.
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p. 481 - 490
(2007/10/02)
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- Azabicyclohexanes
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Substituted 3-azabicyclo[3.1.0]hexanes, acid addition salts, method of use and method of preparation are described. The compounds have anxiolytic and analgesic activity.
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