- Radical 1,4-Aryl Migration Enabled Remote Cross-Electrophile Coupling of α-Amino-β-Bromo Acid Esters with Aryl Bromides
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We report an unprecedented, efficient nickel-catalysed radical relay for the remote cross-electrophile coupling of β-bromo-α-benzylamino acid esters with aryl bromides via 1,4-aryl migration/arylation cascades. β-Bromo-α-benzylamino acid esters are consid
- Chen, Shi-Lu,He, Jin,Hong, Yu,Li, Jin-Heng,Liu, Jian,Liu, Ting,Tang, Shi,Wang, Shuo-Wen,Xu, Zhen-Hua,Yu, Jian
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supporting information
p. 21360 - 21367
(2021/08/23)
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- NOVEL, HIGHLY ACTIVE AMINO-THIAZOLE SUBSTITUTED INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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Page/Page column 80
(2019/05/22)
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- Tertiary-Amine-Based Inhibitors of the Astacin Protease Meprin α
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Metalloproteinases of the astacin family are drawing ever increasing attention as potential drug targets. However, knowledge regarding inhibitors thereof is limited in most cases. Crucial for the development of metalloprotease inhibitors is high selectivi
- Tan, Kathrin,J?ger, Christian,Schlenzig, Dagmar,Schilling, Stephan,Buchholz, Mirko,Ramsbeck, Daniel
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supporting information
p. 1619 - 1624
(2018/07/31)
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- Synthesis and reactivity of tripodal complexes containing pendant bases
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The synthesis of a new tripodal ligand family that contains tertiary amine groups in the second-coordination sphere is reported. The ligands are tris(amido)amine derivatives, with the pendant amines attached via a peptide coupling strategy. They were designed to function as new molecular catalysts for the oxygen reduction reaction (ORR), in which the pendant acid/base group could improve the catalyst performance. Two members of the ligand family were each metalated with cobalt(II) and zinc(II) to afford trigonal-monopyramidal complexes. The reaction of the cobalt complexes [Co(L)]- with dioxygen reversibly generates a small amount of a cobalt(III) superoxo species, which was characterized by electron paramagnetic resonance (EPR) spectroscopy. Protonation of the zinc complex Zn[N{CH2CH2NC(O)CH 2N(CH2Ph)2}3)]- ([Zn(TNBn)]-) with 1 equiv of acid occurs at a primary-coordination-sphere amide moiety rather than at a pendant basic site. The addition of excess acid to any of the complexes [M(L)]- results in complete proteolysis and formation of the ligands H3L. These undesired reactions limit the use of these complexes as catalysts for the ORR. An alternative ligand with two pyridyl arms was also prepared but could not be metalated. These studies highlight the importance of the stability of the primary-coordination sphere of ORR electrocatalysts to both oxidative and acidic conditions.
- Blacquiere, Johanna M.,Pegis, Michael L.,Raugei, Simone,Kaminsky, Werner,Forget, Amelie,Cook, Sarah A.,Taguchi, Taketo,Mayer, James M.
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p. 9242 - 9253
(2014/11/08)
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- Synthesis of aromatic α-aminoesters: Palladium-catalyzed long-range arylation of primary Csp3-H bonds
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Remote control: The title reaction for β-Iζ arylation of α-amino esters with aryl bromides is described. This reaction, which occurs selectively at the terminal position of linear alkyl chains, gives rise to synthetically useful (hetero)arylalanines and homologues after debenzylation (see scheme). Copyright
- Aspin, Sam,Goutierre, Anne-Sophie,Larini, Paolo,Jazzar, Rodolphe,Baudoin, Olivier
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supporting information
p. 10808 - 10811
(2013/01/15)
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- Selective synthesis of either isoindole- or isoindoline-1-carboxylic acid esters by Pd(0)-catalyzed enolate arylation
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Figure presented. Two efficient palladium-catalyzed intramolecular α-arylation reactions of α-amino acid esters have been developed that allow either 1-isoindolecarboxylic acid esters or the corresponding isoindolines to be selectively synthesized simply by a slight change of reaction conditions.
- Sole, Daniel,Serrano, Olga
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supporting information; experimental part
p. 6267 - 6270
(2010/12/19)
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- Preparation of (R)- and (S)-γ-amino-β-hydroxypropylphosphonic acid from glycine
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An efficient synthesis of both enantiomers of γ-amino-β-hydroxypropylphosphonic acid, an analogue of GABOB, has been achieved for the first time starting from glycine, through the resolution of dimethyl (±)-3-(N,N-dibenzylamino)-2-hydroxypropylphosphonate
- Ordonez, Mario,Gonzalez-Morales, Angelina,Ruiz, Cesar,De La Cruz-Cordero, Ricardo,Fernandez-Zertuche, Mario
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p. 1775 - 1779
(2007/10/03)
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- LiOH-mediated N-monoalkylation of α-amino acid esters and a dipeptide ester using activated alkyl bromides
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Selective N-monoalkylation of α-amino esters with activated alkyl bromides was studied using various alkali or alkali earth metal bases. In the production of N-monoalkylated amino ester derivatives and suppression of N,N-dialkylation, lithium hydroxide wa
- Cho, Jong Hyun,Kim, B.Moon
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p. 1273 - 1276
(2007/10/03)
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- Facile synthesis of pyrazino[2,3-e][1,4]diazepine derivatives via the intramolecular aza-Wittig reaction
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Pyrazino[2,3-d][1,4]diazepine derivatives were synthesized from 3-aminopyrazine-2-carboxylic acid 1 and α-amino acid esters via the intramolecular aza-Wittig reaction.
- Okawa, Tomohiro,Eguchi, Shoji
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- New indium-mediated reactions of enamines
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New reactions of enamines were observed with allyl bromide or methyl bromoacetate in the presence of indium powder in THF, yielding respectively homoallylamines and β-aminoesters.
- Bossard, Fabienne,Dambrin, Valery,Lintanf, Valeie,Beuchet, Pierre,Mosset, Paul
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p. 6055 - 6058
(2007/10/02)
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- DIBENZYLAMINOACETATES AS USEFUL SYNTHETIC EQUIVALENTS OF GLYCINE IN THEi SYNTHESIS OF α-AMINO-β-HYDROXYACIDS
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The stereochemical course of three new simple methodologies for the preparation of α-amino-β-hydroxyacids starting from dibenzylaminoacetates as synthetic equivalents of glycine is described.While the aldol-type condensation via lithium enolates gave results highly dependent on the aldehyde employed, producing in some cases diastereoselectivities up to 5:1 for the anti isomers, the acid-catalysed aldol condensation of silyl ketene acetals yielded predominantly syn adducts with selectivities from 5:1 to 32:1.Finally the acylation-reduction procedure gave the best results in terms of yields and stereoselectivities, affording syn isomers with excellent induction ( 13:1).
- Guanti, Giuseppe,Banfi, Luca,Narisano, Enrica,Scolastico, Carlo
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p. 3671 - 3684
(2007/10/02)
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- Alkylation and Condensation Reactions of N,N-Dibenzylglycine Esters: Synthesis of α-Amino Acid Derivatives
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Upon deprotonation N,N-dibenzylglycine esters undergo alkylation and condensation reactions at the α-carbon atom with various electrophiles.
- Gray, Brian D.,Jeffs, Peter W.
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p. 1329 - 1330
(2007/10/02)
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