- Catalytic Strategy for Regioselective Arylethylamine Synthesis
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A mild, modular, and practical catalytic system for the synthesis of the highly privileged phenethylamine pharmacophore is reported. Using a unique combination of organic catalysts to promote the transfer of electrons and hydrogen atoms, this system performs direct hydroarylation of vinyl amine derivatives with a wide range of aryl halides (including aryl chlorides). This general and highly chemoselective protocol delivers a broad range of arylethylamine products with complete regiocontrol. The utility of this process is highlighted by its scalability and the modular synthesis of an array of bioactive small molecules.
- Boyington, Allyson J.,Seath, Ciaran P.,Zearfoss, Avery M.,Xu, Zihao,Jui, Nathan T.
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supporting information
p. 4147 - 4153
(2019/03/07)
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- Iridium-Catalyzed Unreactive C(sp3)-H Amination with 2,2,2-Trichloroethoxycarbonyl Azide
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An additive-assisted iridium-catalyzed directed C(sp3)-H amination with 2,2,2-trichloroethoxycarbonyl azide as an amino source is reported. Both carboxylate anions and the corresponding cations in the additives are crucial to achieve satisfactory efficiency. Sodium acetate or n-pentanoic acid can promote the amination of various primary C(sp3)-H bonds adjacent to secondary, tertiary, and quaternary carbons in ketoximes or N-aromatic heterocycles, respectively, providing a practical route to versatile β-amino ketoxime and N-heteroaryl ethanamine derivatives. The amination products can be treated as isocyanate analogues and can be converted to other useful amino functionalities. An iridacyclic compound was isolated and identified as a plausible intermediate.
- Zhang, Tao,Hu, Xuejiao,Dong, Xunqing,Li, Guigen,Lu, Hongjian
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supporting information
p. 6260 - 6264
(2018/10/02)
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- INHIBITION OF BACTERIAL BIOFILMS WITH ARYL CARBAMATES
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Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
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Page/Page column 33-34
(2012/02/01)
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- 1,3-BENZOTHIAZINONE DERIVATIVES AND USE THEREOF
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This invention provides a compound represented by the formula (I) :wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents;R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents;n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I) , which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
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- Quinolones used as MRS inhibitors and bactericides
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Compounds of formula (I) are inhibitors of the bacterial enzymeS aureusmethionyl tRNA synthetase and are of use in treating bacterial infections.
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- Symmetry-Based Inhibitors of HIV Protease. Structure-Activity Studies of Acylated 2,4-Diamino-1,5-diphenyl-3-hydroxypentane and 2,5-Diamino-1,6-diphenylhexane-3,4-diol
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The structure-activity relationships in two series of novel, symmetry-based inhibitors of HIV protease, the enzyme responsible for maturation of the human immunodeficiency virus, are described.Beginning with lead compounds 3-6, the effect of adding polar, heterocyclic end groups to one or both ends of the symmetric or pseudosymmetric inhibitors was probed.Aqueous solubility was enhanced >1000-fold while maintaining potent inhibition of purified HIV-1 protease and anti-HIV activity in vitro.Pharmacokinetic studies in rats indicated a substantial difference in the absorption properties of mono-ol-based and diol-based inhibitors.The oral bioavailability of inhibitor 19 in rats was 19percent; however, the Cmax obtained failed to exceed the anti-HIV EC50 in vitro.Substantial plasma levels of potent inhibitors of the diol class were not obtained after oral administration in rats; however, the optimal combination of aqueous solubility and in vitro antiviral activity of several inhibitors support their potential use in intravenous therapy.
- Kempf, Dale J.,Codacovi, Lynnmarie,Wang, Xiu Chun,Kohlbrenner, William E.,Wideburg, Norman E.,et al.
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p. 320 - 330
(2007/10/02)
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