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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 ...

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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 ...

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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 ...

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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 ...

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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 ...

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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 ...

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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 ...

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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 ...

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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 ...

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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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