Report of the Stanford Linked Data Workshop

The Stanford University Libraries and Academic Information Resources (SULAIR) with the Council on Library and Information Resources (CLIR) conducted at week-long workshop on the prospects for a large scale, multi-national, multi-institutional prototype of a Linked Data environment for discovery of and navigation among the rapidly, chaotically expanding array of academic information resources. As preparation for the workshop, CLIR sponsored a survey by Jerry Persons, Chief Information Architect emeritus of SULAIR that was published originally for workshop participants as background to the workshop and is now publicly available. The original intention of the workshop was to devise a plan for such a prototype. However, such was the diversity of knowledge, experience, and views of the potential of Linked Data approaches that the workshop participants turned to two more fundamental goals: building common understanding and enthusiasm on the one hand and identifying opportunities and challenges to be confronted in the preparation of the intended prototype and its operation on the other. In pursuit of those objectives, the workshop participants produced:1. a value statement addressing the question of why a Linked Data approach is worth prototyping;2. a manifesto for Linked Libraries (and Museums and Archives and …);3. an outline of the phases in a life cycle of Linked Data approaches;4. a prioritized list of known issues in generating, harvesting & using Linked Data;5. a workflow with notes for converting library bibliographic records and other academic metadata to URIs;6. examples of potential “killer apps” using Linked Data: and7. a list of next steps and potential projects.This report includes a summary of the workshop agenda, a chart showing the use of Linked Data in cultural heritage venues, and short biographies and statements from each of the participants

Silicone-Supported Cinchona Alkaloid Derivatives as Insoluble Organocatalysts in the Enantioselective Dimerization of Ketenes

A straightforward procedure is presented for the covalent immobilization of ester and silyl ether derivatives of the Cinchona alkaloid 10,11-dihydroquinidine within insoluble cross-linked silicone elastomeric films. These materials were effective heterogeneous organocatalysts in the asymmetric dimerization of ketenes, which provided chiral Weinreb β-ketoamides in 28–83 yield and 79–99 ee in the course of several recycles. A productivity/enantioselectivity protocol is also proposed to better assess the relative merits of soluble and supported asymmetric catalytic systems towards process intensification

Synthetic and computational studies on the tricarboxylate core of 6,7-dideoxysqualestatin H5 involving a carbonyl ylide cycloaddition–rearrangement

Reaction of diazodiketoesters 17 and 28 with methyl glyoxylate in the presence of catalytic rhodium(II) acetate generates predominantly the 6,8-dioxabicyclo[3.2.1]octanes 29 and 30, respectively. Acid-catalysed rearrangement of the corresponding alcohol 31 favours, at equilibrium, the 2,8-dioxabicyclo[3.2.1]octane skeleton 33 of the squalestatins–zaragozic acids. Force field calculations on the position of the equilibrium gave misleading results. DFT calculations were correct in suggesting that the energy difference between 31 and 33 should be small, but did not always suggest the right major product. Calculation of the NMR spectra of the similar structures could be used to assign the isomers with a high level of confidence

Structure‐based design, synthesis and biological evaluation of bis‐tetrahydropyran furan acetogenin mimics targeting the trypanosomatid F1 component of ATP synthase

This work was funded by the Leverhulme Trust (G.J.F.), Wellcome Trust ISSF support (G.J.F./T.K.S.) and the European Community’s Seventh Framework Programme under grant agreement No. 602773 [Project KINDRED] (T.K.S.).The protozoan parasites Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp. are responsible for the severely debilitating neglected Tropical diseases of African sleeping sickness, Chagas disease and leishmaniasis, respectively. As part of our ongoing programme exploring the potential of simplified analogues of the acetogenin chamuvarinin we identified the T. brucei FoF1‐ATP synthase as a target of our earlier triazole analogue series. Using computational docking studies we hypothesized that the central triazole heterocyclic spacer could be substituted for a central 2,5‐substituted furan moiety, thus diversifying the chemical framework for the generation of compounds with greater potency and/or selectivity. Here we report the design, docking, synthesis and biological evaluation of new series of trypanocidal compounds and demonstrate their on‐target inhibitory effects. Furthermore, the synthesis of furans by the modular coupling of alkyne‐ and aldehyde‐THPs to bis‐THP 1,4‐alkyne diols followed by ruthenium/xantphos‐catalysed heterocyclisation described here represents the most complex use of this method of heterocyclisation to date.Publisher PDFPeer reviewe

Synthesis and reactions of donor cyclopropanes: efficient routes to cis- and trans-tetrahydrofurans

A detailed study on the synthesis and reactions of silylmethylcyclopropanes is reported. In their simplest form, these donor-only cyclopropanes undergo Lewis acid promoted reaction to give either cis- or trans-tetrahydrofurans, with the selectivity being reaction condition-dependant. The adducts themselves are demonstrated to be an important scaffold for structural diversification. The combination of a silyl-donor group in a donor-acceptor cyclopropane with novel acceptor groups is also discussed

Asenjonamides A–C, antibacterial metabolites isolated from Streptomyces asenjonii strain KNN 42.f from an extreme-hyper arid Atacama Desert soil

Bio-guided fractionation of the culture broth extract of Streptomyces asenjonii strain KNN 42.f recovered from an extreme hyper-arid Atacama Desert soil in northern Chile led to the isolation of three new bioactive ?-diketones; asenjonamides A–C (1–3) in addition to the known N-(2-(1H-indol-3-yl)-2-oxoethyl)acetamide (4), a series of bioactive acylated 4-aminoheptosyl-?-N-glycosides; spicamycins A–E (5–9), and seven known diketopiperazines (10–16). All isolated compounds were characterized by HRESIMS and NMR analyses and tested for their antibacterial effect against a panel of bacteria

Enantioselective Rhodium-Catalyzed Addition of Potassium Alkenyltrifluoroborates to Cyclic Imines

Cyclic imines, in which the C[DOUBLE BOND]N bond is constrained in the Z geometry, have been identified as highly effective substrates for enantioselective rhodium-catalyzed additions of potassium alkenyltrifluoroborates. Not only is the alkene in the products a useful functional handle for subsequent manipulations, products containing aryl sulfamates may be employed in nickel-catalyzed Suzuki–Miyaura and Kumada coupling reactions to generate further compounds of interest