
Shared posts
Oxetanes: Recent Advances in Synthesis, Reactivity, and Medicinal Chemistry
Enantioconvergent catalysis
Abstract
An enantioconvergent catalytic process has the potential to convert a racemic starting material to a single highly enantioenriched product with a maximum yield of 100%. Three mechanistically distinct approaches to effecting enantioconvergent catalysis are identified, and recent examples of each are highlighted. These processes are compared to related, non-enantioconvergent methods.

Beilstein J. Org. Chem. 2016, 12, 2038–2045. doi:10.3762/bjoc.12.192
HPLC-Assisted Automated Oligosaccharide Synthesis: Implementation of the Autosampler as a Mode of the Reagent Delivery
Cobalt-Catalyzed Hydrosilylation/Cyclization of 1,6-Enynes
Determining crystal structures through crowdsourcing and coursework
Determining crystal structures through crowdsourcing and coursework
Nature Communications, Published online: 16 September 2016; doi:10.1038/ncomms12549
Building crystal structures into the electron density is an important step in protein structure solution. Here, the authors recruit online game players, students, and experienced crystallographers to compete in a competition to solve a new structure, and find that crowdsourcing model-building works.
N-Oxides rescue Ru(V) in catalytic Griffith-Ley (TPAP) alcohol oxidations
DOI: 10.1039/C6CC05440D, Communication
Electrochemistry of tetrapropylammonium perruthenate (TPAP) reveals that an unstable Ru(V) complex is reoxidised by amine N-oxides in catalytic Griffith-Ley alcohol oxidations.
The content of this RSS Feed (c) The Royal Society of Chemistry
Copper-Catalyzed Intramolecular Benzylic C–H Amination for the Synthesis of Isoindolinones
Stereoselective Glycosylation of 2-Nitrogalactals Catalyzed by a Bifunctional Organocatalyst
Flow Grignard and Lithiation: Screening Tools and Development of Continuous Processes for a Benzyl Alcohol Starting Material

Development of Specific, Irreversible Inhibitors for a Receptor Tyrosine Kinase EphB3
An histidine covalent receptor and butenolide complex mediates strigolactone perception

Nature Chemical Biology. doi:10.1038/nchembio.2147
Authors: Alexandre de Saint Germain, Guillaume Clavé, Marie-Ange Badet-Denisot, Jean-Paul Pillot, David Cornu, Jean-Pierre Le Caer, Marco Burger, Frank Pelissier, Pascal Retailleau, Colin Turnbull, Sandrine Bonhomme, Joanne Chory, Catherine Rameau & François-Didier Boyer
Alkylation of Sulfonamides with Trichloroacetimidates under Thermal Conditions
Diborane-Mediated Deoxygenation of o-Nitrostyrenes To Form Indoles
A Homogeneous Method for the Conveniently Scalable Palladium- and Nickel-Catalyzed Cyanation of Aryl Halides

Sterically Encumbered Tetraarylimidazolium Carbene Pd-PEPPSI Complexes: Highly Efficient Direct Arylation of Imidazoles with Aryl Bromides under Aerobic Conditions
Synthesis of a Small-Molecule Library with Skeletal Diversity from Hemslecin A via the Reaction-Discovery Strategy
Copper-Catalyzed Enantioselective Addition of Styrene-Derived Nucleophiles to Imines Enabled by Ligand-Controlled Chemoselective Hydrocupration
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease
Resilient British science will withstand Brexit
Resilient British science will withstand Brexit
Nature 535, 7613 (2016). http://www.nature.com/doifinder/10.1038/535467a
Author: Ehsan Masood
UK scientists have had to fight to stay international before, and they must not stop now, says Ehsan Masood.
Mn-, Fe-, and Co-Catalyzed Radical Hydrofunctionalizations of Olefins
Synthesis of Tetrahydroisoquinoline Alkaloids and Related Compounds through the Alkylation of Anodically Prepared α-Amino Nitriles
11-Step Total Synthesis of (−)-Maoecrystal V
MIDA boronates are hydrolysed fast and slow by two different mechanisms

Nature Chemistry. doi:10.1038/nchem.2571
Authors: Jorge A. Gonzalez, O. Maduka Ogba, Gregory F. Morehouse, Nicholas Rosson, Kendall N. Houk, Andrew G. Leach, Paul H.-Y. Cheong, Martin D. Burke & Guy C. Lloyd-Jones
The staged hydrolysis of N-methylimidodiacetic (MIDA) boronates is a prerequisite for their application in small-molecule constructions. Mechanistic studies now show that two distinct hydrolysis mechanisms operate in parallel, the partitioning — which is dependent on the pH, water activity and homogeneity of the medium — can be readily quantified by 18O incorporation.
Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430)
Coinage Metal Hydrides: Synthesis, Characterization, and Reactivity
Design and Applications of an Efficient Amphiphilic “Click” CuI Catalyst in Water

Highly Selective and Modular Synthesis of 3-Aryl-4-(arylethynyl)-2H-chromen-2-ones from 2-Iodoaryl 2-Arylacetates through a Carbonylative Sonogashira Coupling–Intramolecular Aldol Cascade Reaction
A modular method for the synthesis of 3-aryl-4-(arylethynyl)-2H-chromen-2-ones from 2-iodoaryl 2-arylacetates and arylacetylenes has been developed. The carbonylative Sonogashira coupling–intramolecular aldol casade reaction was carried out in the presence of Pd(PPh3)2(Cl)2 as the catalyst. The one-pot approach that involves the in situ formation of the 2-iodoaryl 2-arylacetates from the corresponding 2-iodophenols and 2-arylacetyl chlorides followed by the palladium-catalyzed carbonylative annulation in the presence of the arylacetylene has also been described for the formation of the 3-aryl-4-(arylethynyl)-2H-chromen-2-ones.

A modular approach for the synthesis of 3-aryl-4-(arylethynyl)-2H-chromen-2-ones from iodoaryl 2-arylacetates and arylacetylenes has been developed. This highly selective general method was used to prepare 24 different 3,4-disubstitued 2H-chromen-2-one derivatives in good to excellent yields.


















