Org. and Biomol. Chem.

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Updated: 2 hours 9 min ago

An efficient total synthesis of leukotriene B4

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00473J, PaperKaroline Gangestad Primdahl, Jorn Eivind Tungen, Marius Aursnes, Trond Vidar Hansen, Anders Vik
Lipid mediators have attracted a great interest from scientist within the chemical, medicinal, and pharmaceutical research community. One such example is leukotriene B4 which has been the subject of many...
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Metal-Free Cascade Cyclization of Alkenes toward Polyfluorinated Oxindoles

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00454C, PaperShi Tang, Zhi-Hao Li, Ming-Wei Wang, Zhi Ping Li, Rui Long Sheng
A simple AIBN-mediated cyclization reaction of activated alkenes toward perfluorinated was developed. In the presence of readily available AIBN, N-arylacrylamide and perfluoroalkyl iodides underwent perfluorination reaction to give perfluoroinated oxindoles...
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Stereogenic [small alpha]-carbons determine the shape and topology of [13]-macrodilactones

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00402K, CommunicationAnniefer Magpusao, Kelli Rutledge, Brandon Mercado, Mark Peczuh
The configuration of [small alpha]-stereogenic centers affects the shape and topology of [13]-macro-dilactones. When one [small alpha]-stereogenic center is substituted, it directs the planar chirality of the macrocycle; when two centers are...
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Influence of non-covalent preorganization on supramolecular effective molarities

2 hours 9 min ago

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C5OB00231A, PaperOpen Access Open Access Creative Commons Licence&nbsp This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Hongmei Sun, Cristina Navarro, Christopher A. Hunter
Formation of H-bonding interactions, which restrict the conformational mobility of a flexible linker, have no effect on chelate cooperativity in a family of porphyrin-pyridine complexes.
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Efficient approach to 2-hydroxy-2,3-dihydrofuran derivatives and its application for the synthesis of novel 4-(1H-pyrazol-4-yl)pyridazines

2 hours 9 min ago

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C5OB00163C, PaperJun-Rui Ma, Wen-Ming Shu, Kai-Lu Zheng, Fan Ni, Guo-Dong Yin, An-Xin Wu
A highly efficient method for the synthesis of 2-hydroxy-2,3-dihydrofuran derivatives from 1,4-enediones and phenacyl pyridinium halides via a domino reaction has been developed. At the same time, we also synthesize the novel 4-(1H-pyrazol-4-yl)pyridazine skeleton.
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Gold-catalysed glycosylation reaction using an easily accessible leaving group

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00248F, CommunicationSrinivasa Rao Koppolu, Ramana Nidanna, Balamurugan Rengarajan
Gold(III)-catalysed glycosylation reaction has been developed by employing a new and easily accessible leaving group synthesized from ethyl cyanoacetate. Several nucleophiles like alcohols, thiols, allyltrimethylsilane, trimethylsilyl azide and triethylsilane have...
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Contribution of dihydrouridine in folding of the D-arm in tRNA

2 hours 9 min ago

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C5OB00164A, PaperN. Dyubankova, E. Sochacka, K. Kraszewska, B. Nawrot, P. Herdewijn, E. Lescrinier
NMR studies of the D-arm of tRNAiMet revealed the crucial role of dihydrouridine nucleoside in folding of the oligo.
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Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00474H, PaperHerman S. Overkleeft, Nora Liu, Sascha Hoogendoorn, Bas van der Kar, Allard Kaptein, Tjeerd Barf, Christoph Driessen, Dmitri Filippov, Gijsbert A van der Marel, Mario van der Stelt
Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) and has been approved for the treatment of haematological malignancies, such as chronic lymphocytic leukaemia, mantle cell lymphoma...
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Palladium-Catalyzed Carbonylative Sonogashira Coupling between Aryl Triazenes and Alkynes

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00502G, CommunicationXiao-Feng Wu, Wanfang Li
We disclosed a palladium-catalyzed carbonylative Sonogashira reaction with aryl triazenes and alkynes as substrates and methanesulfonic acid as the additive. A series of [small alpha],[small beta]-ynones were synthesized by this alternative procedure....
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Semi-synthesis of thioamide containing proteins

2 hours 9 min ago

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C5OB00224A, PerspectiveYanxin J. Wang, D. Miklos Szantai-Kis, E. James Petersson
To make thioamide protein folding experiments applicable to full-sized proteins, our laboratory has used a combination of native chemical ligation of thiopeptide fragments, unnatural amino acid mutagenesis to install fluorophore partners in expressed protein fragments, and chemoenzymatic protein modification to render these expressed protein ligations traceless.
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Convenient synthesis of deazaflavin cofactor FO and its activity in F420-dependent NADP reductase

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00365B, CommunicationMohammad S. Hossain, Cuong Q. Le, Ebenezer Joseph, Toan Q. Nguyen, Kayunta Johnson-Winters, Frank Foss
F420 and FO are phenolic 5-deazaflavin cofactors that complement nicotinamide and flavin redox cofactors in biochemical oxidoreductases and photocatalytic systems. Specifically, these 5-deazaflavins lack the single electron reactivity of riboflavin-derived...
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Triazolophostins: A Library of Novel and Potent Agonists of IP3 Receptors

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00440C, PaperKana M Sureshan, Amol Madhukar Vibhute, Colin W Taylor, Vera Konieczny
IP3 receptors are channels that mediate release of Ca2+ from the intracellular stores of cells stimulated by hormones or neurotransmitters. Adenophostin A (AdA) is the most potent agonist of IP3...
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Isostructural Re(I)/99mTc(I) Tricarbonyl Complexes Functionalized with Benzothiazole Derivatives for Cancer Theranostics

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00124B, PaperPatrique Nunes, Goreti Ribeiro Morais, Elisa Palma, Francisco Silva, Maria Cristina Oliveira, Vera F. C. Ferreira, Filipa Mendes, Lurdes Gano, Hugo Vicente Miranda, Tiago F. Outeiro, Isabel Santos, Antonio Paulo
Merging classical organic anticancer drugs with metal-based compounds in one single molecule offers the possibility of exploring new approaches for cancer theranostics, i.e., the combination of diagnostic and therapeutic modalities....
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Palladium(II)-catalyzed intramolecular carboxypalladation-olefin insertion cascade: direct access to indeno[1,2-b]furan-2-ones

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00458F, PaperVellaisamy Sridharan, Perumal Vinoth, Thavaraj Vivekanand, Padmakar A. Suryavanshi, J. Carlos Menendez, Hiroaki Sasai
A catalytic, atom-economical, domino 5-endo-dig cyclization-intramolecular olefin insertion sequence was developed under mild conditions. Aryl alkynoic acids bearing a tethered enone partner afforded the indeno[1,2-b]furan-2-ones, the core skeleton present in...
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Cobalt (II) catalyzed C(sp)-H bond functionalization of alkynes with phenyl hydrazines: A facile access to diaryl 1,2-diketones

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00419E, PaperJaideep B Bharate, Sheenu Abbat, Rohit Sharma, Prasad. V. Bharatam, Ram A Vishwakarma, Sandip Bibishan Bharate
A cobalt acetylacetonate catalyzed oxidative diketonation of alkynes via C(sp)-H bond functionalization has been described. The reaction involves a free-radical mechanism, wherein the phenyl radical formed from phenyl hydrazine couples...
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Divergent, Stereoselective Access to Heterocyclic [small alpha],[small alpha]-Quaternary- and [small beta]2,3,3-Amino Acid Derivatives from a N-Pmp-protected Orn-Derived [small beta]-Lactam

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00429B, PaperDiego Nunez-Villanueva, Maria teresa Garcia-Lopez, Mercedes Martin-Martinez, Rosario Gonzalez-Muniz
A suitably protected Orn-derived (3S,4S)-[small beta]-lactam was used as common intermediate in the synthesis of conformationally constrained (3S,4S)-2-oxoazepane [small alpha],[small alpha]- and (2S,3S)-2-oxopiperidine-[small beta]2,3,3-amino acid derivatives. Compared to the alternative procedures using an N-p-methoxybenzyl...
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C5-Azobenzene-functionalized locked nucleic acid uridine: isomerization property, hybridization ability, and enzymatic stability

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00477B, PaperKunihiko Morihiro, Osamu Hasegawa, Shohei Mori, Shin-ichi Tsunoda, Satoshi Obika
Oligonucleotides (ONs) modified with locked nucleic acid (LNA) are widely used in the fields of therapeutics, diagnosis, and nanotechnology. There has been significant effort towards developing LNA analogues bearing modified...
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Mild One-Pot Horner-Wadsworth-Emmons Olefination and Intramolecular N-arylation for the Syntheses of Indoles, All Regio-isomeric Azaindoles, and Thienopyrroles

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00528K, PaperJi hye choi, hwan jung lim
The syntheses of various N-protected aromatic-ring fused pyrrole-2-carboxylate derivatives have been accomplished using mild one-pot Horner-Wadsworth-Emmons olefination and Cu-catalyzed intramolecular N-arylation reactions. The optimized mild one-pot reaction conditions of various...
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Synthesis of 6,8-9 Poly-substituted Purine Analogue Libraries as Pro-Apoptotic Inducers of Human Leukemic Lymphocytes and DAPK-1 Inhibitors.

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00230C, PaperMaria Jose Pineda de las Infantas, Sara Torres-Rusillo, Juan Diego Unciti-Broceta, Pablo Fernandez-Rubio, Angelica Luque-Gonzalez, Miguel Angel Gallo, Ignacio J Molina, Asier Uniciti Broceta, Juan J. Diaz-Mochon
A 18-member library of 6,8,9-poly-substituted purines was prepared from pyrimidines, primary alcohols and N,N-dimethylamides under basic conditions via a novel one-pot synthetic pathways controlled by amide sizes and the novel...
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Novel ferrocene-based bifunctional amine-thioureas for asymmetric Michael addition of acetylacetone to nitroolefins

2 hours 9 min ago
Org. Biomol. Chem., 2015, Accepted Manuscript
DOI: 10.1039/C5OB00298B, Paperxiaochen ren, chunyan he, yingle feng, Yonghai Chai, weiping chen, shengyong zhang, Wei Yao
An efficient method was developed to synthesize the ferrocene-based bifunctional amine-thioureas bearing multiple hydrogen-bonding donors. Asymmetric Michael addition of acetylacetone to nitroolefins catalyzed by these novel bifunctional catalysts afford the...
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