Royal Society of Chemistry

Syntheses of arabinose-derived pyrrolidine catalysts and their applications in intramolecular Diels-Alder reactions

Org. and Biomol. Chem. - 17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB02219J, PaperTony K. M. Shing, Kwun W. Wu, Ho T. Wu, Qicai Xiao
Six hydroxylated pyrrolidine catalysts were synthesized from D-arabinose and applied to asymmetric intramolecular Diels-Alder reactions with concomitant desymmetrization.
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[small beta]-Ketothioamides: efficient reagents in synthesis of heterocycles

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02024C, Review ArticleWei-Si Guo, Li-Rong Wen, Ming Li
[small beta]-ketothioamides (KTAs) are versatile building blocks for the rapid construction of various heterocyclic compounds. In the past decade, a number of successful reactions based on KTAs have been developed for...
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Asymmetric metal free [small beta]-boration of [small alpha],[small beta]-unsaturated imines assisted by (S)-MeBoPhoz

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02478H, CommunicationElena Fernandez, Andrew Whiting, Xavier Sanz, Carles Bo, Enrico LaCascia
The adduct [MeO[rightward arrow]Bpin-Bpin]- efficiently mediates the [small beta]-boration of [small alpha],[small beta]-unsaturated imines formed "in situ". The use of chiral phosphines as additives, and in particular the chiral phosphine (S)-MeBoPhoz, enables the catalytic...
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Synthesis and physico-chemical properties of the first water soluble Cu(II)@hemicryptophane complex

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02085E, PaperAlexandre Martinez, Aline schmitt, CHRISTOPHE BUCHER, Vincent MAUREL, Jean-Pierre Dutasta, Solene Collin
A hemicryptophane ligand soluble in water at neutral pH was obtained thanks to the derivatization of the cyclotribenzylene unit with three carboxylate groups. The corresponding Cu(II) complex was then synthesized...
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Bacterial Patterning Controlled by Light Exposure

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02483D, CommunicationWillem Velema, Jan Pieter Van der Berg, Wiktor C Szymanski, Arnold Driessen, Ben L Feringa
Patterning of multiple bacterial strains in one system is achieved by employing a single photo-activated antibiotic. Varying the light-exposure time results in zones with mixed and single populations.
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E- or Z-Selective synthesis of 4-fluorovinyl-1,2,3-triazoles with fluorinated second-generation Julia-Kocienski reagents

Org. and Biomol. Chem. - 17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB02179G, PaperRakesh Kumar, Govindra Singh, Louis J. Todaro, Lijia Yang, Barbara Zajc
Second-generation Julia-Kocienski reagents from CuAAC reactions of [small alpha]-fluoropropargyl benzothiazole sulfone with azides, react with aldehydes and ketones to give N-substituted 4-(1-fluorovinyl)triazoles. Reactions of aldehydes can be tuned towards E or Z-alkenes selectively.
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Recent advances in development of imidazo[1,2-a]pyrazines: synthesis, reactivity and their biological applications

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB01380H, Review ArticleKamal Deep Paul, Vijay Luxami, Richa Goel
Imidazo[1,2-a]pyrazine acts as a versatile scaffold in organic synthesis and drug development. This review article is an effort to compile the progress in synthetic methods and to illustrate its reactivity...
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Near-instant surface-selective fluorogenic protein quantification using sulfonated triarylmethane dyes and fluorogen activating proteins

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02309A, PaperQi Yan, Brigitte Schmidt, Lydia A Perkins, Matharishwan Naganbabu, Saumya Saurabh, Susan Andreko, Marcel Bruchez
Agonist-promoted G-protein coupled receptor (GPCR) endocytosis and recycling plays an important role in many signaling events in the cell. However, the approaches that allow fast and quantitative analysis of such...
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Stereoselective synthesis of fluorinated aminoglycosyl phosphonates

Org. and Biomol. Chem. - 17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB02317J, CommunicationSanne Bouwman, Romano V. A. Orru, Eelco Ruijter
We report the highly stereoselective addition of lithiated difluorophosphonates to nitroglycals, providing synthetic access to biologically relevant fluorinated aminoglycosyl phosphonates.
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Synthesis and antimalarial evaluation of amide and urea derivatives based on the thiaplakortone A natural product scaffold

Org. and Biomol. Chem. - 17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01849D, PaperBrett D. Schwartz, Tina S. Skinner-Adams, Katherine T. Andrews, Mark J. Coster, Michael D. Edstein, Donna MacKenzie, Susan A. Charman, Maria Koltun, Scott Blundell, Anna Campbell, Rebecca H. Pouwer, Ronald J. Quinn, Karren D. Beattie, Peter C. Healy, Rohan A. Davis
A series of amide and urea analogues based on the thiaplakortone A natural product scaffold were synthesised and screened for in vitro antimalarial activity.
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Linear dialdehydes as promising substrates for aminocatalyzed transformations

Org. and Biomol. Chem. - 17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01805B, Review ArticleIndresh Kumar, Panduga Ramaraju, Nisar A. Mir, Anoop Singh
Linear dialdehydes: This article summarizes the recent utilization of linear dialdehydes as appropriate substrates for amine catalyzed cascade/domino transformations.
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Synthesis and antitumor activity of novel 2-substituted indoline imidazolium salt derivatives

Org. and Biomol. Chem. - 17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB02385D, PaperXiao-Liang Xu, Chun-Lei Yu, Wen Chen, Ying-Chao Li, Li-Juan Yang, Yan Li, Hong-Bin Zhang, Xiao-Dong Yang
A series of novel 2-substituted indoline imidazolium salt derivatives were synthesized and their antitumor structure-activity relationship studies were reported.
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Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity

Org. and Biomol. Chem. - 17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01865F, PaperJing Ren, Min Yang, Hongchun Liu, Danyan Cao, Danqi Chen, Jian Li, Le Tang, Jianhua He, Yue-Lei Chen, Meiyu Geng, Bing Xiong, Jingkang Shen
Various 3,8-diaminoimidazo[1,2-a]pyrazines were efficiently prepared by MCR and some products showed moderate Hsp90 inhibitory activity.
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N-Phosphonyl /Phosphinyl Imines and Group-Assisted Purification (GAP) Chemistry/Technology

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02254H, Review ArticleGuanghui An, Cole Seifert, Guigen Li
The development of environmentally benign, operationally simple, and economically viable synthetic methodologies has been a great challenge in organic synthesis. Group-Assisted Purification (GAP) chemistry was established to enable the synthesis...
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1H chemical shift differences of Prelog-Djerassi lactone derivatives: DFT and NMR conformational studies.

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02446J, PaperMarco AB Ferreira, Tulio Jardini Aimola, Dimas Jose da Paz Lima, Luiz Carlos Dias, Claudio Francisco Tormena
This work reports an experimental and theoretical study of the conformational preferences of several Prelog-Djerassi lactone derivatives, to elucidate the 1H NMR chemical shift differences in the lactonic core that...
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Chemoselective Efficient Synthesis of Functionalized [small beta]-oxonitriles through Cyanomethylation of Weinreb Amides

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02398F, CommunicationAshenafi Damtew Mamuye, Laura Castoldi, Ugo Azzena, Wolfgang Holzer, Vittorio Pace
A synthesis of [small beta]-oxonitriles is reported via the generation of R1R2CLiCN species followed by the trapping with variously decorated Weinreb amides. The optimization study revealed that lithiation of acetonitriles is...
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Regulating the cytoprotective response in cancer cells using simultaneous inhibition of Hsp90 and Hsp70.

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02531H, PaperYao Wang, Shelli Renee McAlpine
Both heat shock protein 90 and 70 (Hsp90, Hsp70) are cytoprotective proteins that regulate cell death by stabilizing and folding proteins. Taking a two-pronged approach involving simultaneous inhibition of Hsp90...
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In Tandem or Alone: a Remarkably Selective Transfer Hydrogenation of Alkenes Catalyzed by Ruthenium Olefin Metathesis Catalysts

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02480J, PaperKarol Grela, Grzegorz Krzysztof Zielinski, Cezary Samojlowicz, Tomasz Wdowik
A system for transfer hydrogenation of alkenes, composed from a ruthenium metathesis catalyst and HCOOH is presented. This operationally simple system can be formed directly after a metathesis reaction to...
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Synthesis of Novel Polyhydroxylated Pyrrolidine-Triazole/-Isoxazole Hybrid Molecules

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB01934B, PaperCheng-Kun Lin, Li-Wei Cheng, Huang-Yi Li, wen-Yi Yun, wei-chieh cheng
A straightforward synthesis of novel, 2-heterocyclyl polyhydroxylated pyrrolidines is described. Stereocontrolled additions of nucleophiles to cyclic nitrones generated the corresponding 2,3-trans adducts, allowing the synthesis of the corresponding pyrrolidines via...
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Enabling the (3+2) cycloaddition reaction in assembling newer anti-tubercular lead acting through the inhibition of Gyrase ATPase domain: Lead optimization and structure activity profiling

Org. and Biomol. Chem. - 17 December, 2014 - 22:54
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02049A, PaperJeankumar U Variam, Reshma R Srilakshmi, Renuka Janupally, Brahmam Medapi, Shalini Saxena, Jonnalagadda Padma Sridevi, Pushkar Kulkarni, Perumal Yogeeswari, Dharmarajan Sriram
DNA Gyrase, the sole type II topoisomerase present in Mycobacterium tuberculosis is absent in DNA Gyrase, the sole type II topoisomerase present in Mycobacterium tuberculosis is absent in humans and...
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