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9.059 Aktuelle Fachpublikationen in Organic & Biomolecular Chemistry


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The discovery of a freezing-induced peptide ligation during the total chemical synthesis of human interferon-ε

03.07.2018 | Yin-He Yang; Bin Di; Da-Song Yang, Organic & Biomolecular Chemistry, 2018

A counterintuitive freezing-induced peptide ligation was discovered in the total synthesis of human interferon-ε (hIFN-ε) which blocks HIV infection through unique mechanisms. The successful synthesis of hIFN-ε (187 amino acids) in this research laid the foundation for related anti-AIDS drug ...


Copper-catalyzed oxidative cross-dehydrogenative coupling of 2H-chromenes and terminal alkynes

03.07.2018 | Fei Yang; Yangshan Li; Paul E. Floreancig; Xiaoyan Li; Lei Liu, Organic & Biomolecular Chemistry, 2018

An efficient copper-catalyzed cross-dehydrogenative coupling of 2H-chromenes and terminal alkynes mediated by DDQ has been established. A protic additive, EtOH, proved to be crucial for harmonizing the oxidation with a subsequent alkynylation step by retaining the oxidation state of an ...


An elusive thermal [2 + 2] cycloaddition driven by visible light photocatalysis: tapping into strain to access C2-symmetric tricyclic rings

03.07.2018 | Kamaljeet Singh; Winston Trinh; Jimmie D. Weaver, Organic & Biomolecular Chemistry, 2018

A mild and operationally simple methodology is reported for the synthesis of cyclobutane rings imbedded within a C2-symmetric tricyclic framework. The method uses visible light and an iridium-based photocatalyst to drive the oft-stated “forbidden” thermal [2 + 2] cycloaddition of cycloheptenes ...


Direct C-OH/P(O)-H Dehydration Coupling Forming Phosphine Oxides

03.07.2018 | Long Chen; Yueyue Zhu; Tieqiao Chen; Long Liu; Ji-Shu Zhang; Li-Biao Han, Organic & Biomolecular Chemistry, 2018

A t-BuONa-mediated C-OH/P(O)-H cross dehydration coupling to produce alkylphosphine oxides is developed. This reaction employed the readily available alcohols and P(O)-H compounds as the starting materials, providing an efficient alternative method for constructing sp3C-P bonds. A reasonable ...


Inhibition of the Prototropic Tautomerism in Chrysazine by p-Sulfonatocalixarene Hosts

03.07.2018 | Poojan Milan Gharat; Dilip Kumar Maity; Haridas Pal; Sharmistha Dutta Choudhury, Organic & Biomolecular Chemistry, 2018

This study explores the interesting effect of p-sulfonatocalix[n]arene hosts (SCXn) on the excited-state tautomeric equilibrium of Chrysazine (CZ), a model antitumour drug molecule. Detailed photophysical investigations reveal that conversion of CZ from its excited normal form (N*) to the ...


Carbenium ion formation by fragmentation of electrochemically generated oxonium ions

03.07.2018 | Anna Lielpetere; Aigars Jirgensons, Organic & Biomolecular Chemistry, 2018

Fragmentation of electrochemically generated oxonium ions can be exploited to form carbenium ions at low oxidation potential in the presence of a nuclephile. The application of this concept is demonstrated for allylation of carbenium ions generated by anodic oxidation of ...


Evaluation of Topologically Distinct Constrained Antimicrobial Peptides with Broad-Spectrum Antimicrobial Activity

03.07.2018 | Fang Yuan; Yuan Tian; Weirong Qin; Jingxu Li; Dan Yang; Bing-Chuan Zhao; Feng Yin; Zigang Li, Organic & Biomolecular Chemistry, 2018

Antimicrobial peptides (AMPs) are short cationic peptides with a high affinity for membranes and emerged as a promising therapeutic approach with potential for treating infectious diseases. Chemical stabilization of short peptides proved to be a successful approach for enhancing their ...


Lasso peptides: chemical approaches and structural elucidation

03.07.2018 | Helena Martin-Gómez; Judit Tulla-Puche, Organic & Biomolecular Chemistry, 2018

The discovery and development of novel constrained peptides that combine the advantages of therapeutic proteins with those of small molecules has partially prompted the re-emergence of peptides as therapeutics. In this regard, lasso peptides are characterized by both the selectivity and potency ...


Synthesis of hydrophilic HYNIC-[1,2,4,5]tetrazine conjugates and their use in antibody pretargeting with 99mTc

03.07.2018 | María Fernanda García; Fabio Gallazzi; Mara de Souza Junqueira; Marcelo Fernández; Ximena Camacho; J ..., Organic & Biomolecular Chemistry, 2018

Pretargeted imaging, based on the highly reactive process between [1,2,4,5]tetrazines with trans-cyclooctene (TCO), appears as an attractive strategy to overcome disadvantages associated with traditional radioimmunoconjugates. To be successful, the radiolabeled component should react in vivo with ...


Palladium catalyzed stereocontrolled synthesis of C-aryl glycosides using glycals and arenediazonium salts at room temperature

03.07.2018 | Jeyakumar Kandasamy; Adesh Kumar Singh, Organic & Biomolecular Chemistry, 2018

A stereocontrolled synthesis of aryl-C-glycosides was achieved using glycals and aryldiazonium salts in the presence of palladium acetate. A wide range of glycals including D-glucal, D-galactal, L-rhamanal, D-xylal and D-ribal underwent C-arylation at the anomeric carbon in the presence of ...


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