Results 51 to 60 of about 27,695 (265)

Derivatisable cyanobactin analogues : a semisynthetic approach [PDF]

open access: yes, 2015
This work was supported by the European Research Council (339367), UK Biotechnology and Biological Sciences Research Council (K015508/1) and the Wellcome Trust (Triple TOF 5600 mass spectrometer (094476), the MALDI TOF-TOF Analyser (079272AIA), 700 NMR ...
Naismith, Jim   +18 more
core   +1 more source

Hyperpolarization of [1‐13C]Ketoisocaproate‐d2 by Reversible Exchange with Parahydrogen Enables Profiling of Branched‐Chain‐Amino‐Acid Metabolism in Cellulo and in Vivo

open access: yesAdvanced Science, EarlyView.
We report the fast generation of biocompatible solutions of highly 13C‐hyperpolarized (≈11%) partially‐deuterated ketoisocaproate within <6 min using spin‐lock‐induced crossing and reversible exchange with parahydrogen (SLIC‐SABRE). This enables rapid detection of branched‐chain‐amino‐acid transferase 1 (BCAT1) protein expression and investigation of ...
Stefan Petersen   +18 more
wiley   +1 more source

Syntheses and medicinal chemistry of spiro heterocyclic steroids

open access: yesBeilstein Journal of Organic Chemistry
There is compelling evidence that incorporating a heterocyclic moiety into a steroid can alter its pharmacological and pharmacokinetic properties, driving intense interest in the synthesis of such hybrids among research groups. In this review, we present
Laura L. Romero-Hernández   +5 more
doaj   +1 more source

Discovery of 4,5-Dihydro-1H-thieno[2′,3′:2,3]thiepino [4,5-c]pyrazole-3-carboxamide Derivatives as the Potential Epidermal Growth Factor Receptors for Tyrosine Kinase Inhibitors

open access: yesMolecules, 2018
The epidermal growth factor receptors (EGFRs), in which overexpression (known as upregulation) or overactivity have been associated with a number of cancers, has become an attractive molecular target for the treatment of selective cancers. We report here
Jia Ke   +8 more
doaj   +1 more source

Transfer learning for Heterocycle Synthesis Prediction [PDF]

open access: yes
Heterocycles are important scaffolds in medicinal chemistry that can be used to modulate the binding mode as well as pharmacokinetic properties of drugs.
Dominik, Miketa   +8 more
core   +2 more sources

Calcium‐Mechanochemistry Enabled Ketone Synthesis From Organic Iodides and Carboxylic Acids

open access: yesAdvanced Science, EarlyView.
Mechanochemically generated organocalcium species display unusual chemoselectivity toward carboxylates, enabling direct ketone synthesis without overaddition. Ball milling activates commercial calcium metal under ambient, solvent‐minimized conditions, providing a broad substrate scope, high functional‐group tolerance, and a practical one‐step ...
Mengyao Pei   +9 more
wiley   +1 more source

Convenient Synthesis of Thiohydantoins, Imidazole-2-thiones and Imidazo[2,1-b]thiazol-4-iums from Polymer-Supported α-Acylamino Ketones

open access: yesMolecules, 2018
The preparation of 5-methylene-thiohydantoins using solid-phase synthesis is reported in this paper. After sulfonylation of immobilized Ser (t-Bu)-OH with 4-nitrobenzenesulfonyl chloride followed by alkylation with various bromoketones, the 4-Nos group ...
Petra Králová   +3 more
doaj   +1 more source

Palladium-catalysed heterocycle synthesis [PDF]

open access: yes, 2012
Chapter 1 is a literature review of selected palladium-catalysed aryl C-N and C-S bond forming reactions. The application of these reactions to the synthesis of heterocycles is also discussed.
Sadig, Jessie E.R.
core   +1 more source

Pd‐Catalyzed Asymmetric Dearomative Heck/Tsuji‐Trost Difunctionalization of Naphthalenes

open access: yesAdvanced Science, EarlyView.
We have developed a palladium‐catalyzed asymmetric dearomative Heck/Tsuji‐Trost 1,4‐difunctionalization reaction of naphthalenes, affording 4‐aminospirocyclohexene oxindole products bearing two remote chiral centers. Through the effect of the newly designed chiral sulfinamide phosphine ligand with large steric hindrance, side reactions are inhibited ...
Long‐Ling Ma   +3 more
wiley   +1 more source

Iodine-Catalyzed Diversity-Oriented Synthesis of 3,4-Heterocycle-Fused Coumarins from 4‑Aminocoumarins and Aurones in Different Solvent

open access: yes
An unprecedented protocol has been developed for the synthesis of 3,4-heterocycle-fused coumarins from 4-aminocoumarins and aurones through iodine-catalyzed cascade reactions.
Lin Ma (23007)   +7 more
core   +1 more source

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