Results 91 to 100 of about 25,392 (338)

Transaminase triggered aza-Michael approach for the enantioselective synthesis of piperidine scaffolds [PDF]

open access: yes, 2016
The expanding “toolbox” of biocatalysts opens new opportunities to redesign synthetic strategies to target molecules by incorporating a key enzymatic step into the synthesis.
Andrew Gomm   +6 more
core   +3 more sources

Pharmaceuticals Made with Hydrogen: A Sustainable and Efficient Approach Using Flow Synthesis

open access: yesChemistry – A European Journal, EarlyView.
We demonstrate a sustainable strategy for pharmaceutical manufacturing by combining hydrogen, heterogeneous catalysis, and continuous flow synthesis. The development of novel catalysts and their application in a multi‐step synthesis of donepezil enabled a highly productive process with no intermediate purification.
Shū Kobayashi, Haruro Ishitani
wiley   +1 more source

Base-catalyzed reactions of environmentally relevant N-chloro-piperidines. A quantum-chemical study [PDF]

open access: yes, 2011
Electronic structure methods have been applied to calculate the gas and aqueous phase reaction energies for base-induced rearrangements of N-chloropiperidine, N-chloro-3-(hydroxymethyl)piperidine, and N-chloro-4-4-fluorophenyl)-3-(hydroxymethyl ...
Sakic, Davor   +2 more
core   +1 more source

Highly Potent Fluorogenic Ligands for Triplex DNA: 5‐Substituted 2‐(Naphthalen‐2‐yl)‐4H‐Chromen‐4‐Ones

open access: yesChemistry – A European Journal, EarlyView.
5‐Substituted 2‐(naphthalen‐2‐yl)‐4H‐chromen‐4‐ones are reported as a novel class of highly potent and selective triplex DNA ligands. These ligands induce triplex formation at submicromolar concentrations and inhibit enzymatic activity via ligand‐mediated triplex formation.
Nghia Tran   +4 more
wiley   +1 more source

Opportunities and challenges for direct C–H functionalization of piperazines

open access: yesBeilstein Journal of Organic Chemistry, 2016
Piperazine ranks within the top three most utilized N-heterocyclic moieties in FDA-approved small-molecule pharmaceuticals. Herein we summarize the current synthetic methods available to perform C–H functionalization on piperazines in order to lend ...
Zhishi Ye, Kristen E. Gettys, Mingji Dai
doaj   +1 more source

New One-Pot Methodologies for the Modification or Synthesis of Alkaloid Scaffolds

open access: yesMarine Drugs, 2010
There are several avenues by which promising bioactive natural products can be produced in sufficient quantities to enable lead optimization and medicinal chemistry studies. The total synthesis of natural products is an important, but sometimes difficult,
Amir E. Wahba, Mark T. Hamann
doaj   +1 more source

Nickel-Catalyzed Asymmetric Reductive Cross-Coupling between Heteroaryl Iodides and α-Chloronitriles [PDF]

open access: yes, 2015
A Ni-catalyzed asymmetric reductive cross-coupling of heteroaryl iodides and α-chloronitriles has been developed. This method furnishes enantioenriched α,α-disubstituted nitriles from simple organohalide building blocks.
Kadunce, Nathaniel T., Reisman, Sarah E.
core   +4 more sources

C‐Terminal Nucleobase Modification Amplifies Peptide‐Mediated Liposome Fusion

open access: yesChemistry – A European Journal, EarlyView.
Let's come together right now. Cationic peptides are known to promote aggregation of negatively charged liposomes through electrostatic interaction. The process is reversible: once neutrality is achieved, liposomes disaggregate. Here, we demonstrate that end‐capping peptides with nucleobases turns the process into irreversible fusion.
Laura Morbiato   +4 more
wiley   +1 more source

First asymmetric synthesis of piperidine alkaloid (-)-morusimic acid D [PDF]

open access: yes, 2008
The first asymmetric synthesis of (-)-morusimic acid D, a 2,3-trans-2,6-cis-2-methyl-6-substituted piperidin-3-ol containing alkaloid is reported. The key steps are the reductive alkylation of N,O-diprotected 3-hydroxyglutarimide, a stepwise reductive ...
Huang, Pei-Qiang   +4 more
core   +1 more source

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