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96 Newest Publications about the topic parallel synthesis


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High Throughput Mechanochemistry: Application to Parallel Synthesis of Benzoxazines

10-Jan-2018 | Katia Martina; Laura Rotolo; Andrea Porcheddu; Francesco Delogu; Stephen Bysouth; Giancarlo Cravotto; Evelina Colacino, Chemical Communication, 2018

We describe herein an unprecedented mechanochemical “parallel synthesis” of 3,4-dihydro-2H-benzo[e][1,3]oxazine derivatives via a one pot three component reaction. The new milling system uses a multiposition jar (variable sizes are possible), allowing to process up to 12 samples simultaneously, ...


Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold

05-Sep-2017 | Kelly A. Teske; Ganesha Rai; Premchendar Nandhikonda; Preetpal S. Sidhu; Belaynesh Feleke; Anton Simeonov; Adam Yasg ..., Journal of Combinatorial Chemistry, 2017

We describe the parallel synthesis of novel analogs of GW0742, a peroxisome proliferator-activated receptor δ (PPARδ) agonist. For that purpose, modified reaction conditions were applied, such as a solid-phase palladium-catalyzed Suzuki coupling. In addition, tetrazole-based compounds were ...


Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications

01-Mar-2017 | János Galambos; Attila Bielik; Mikhail Krasavin; Zoltán Orgován; György Domány; Katalin Nógrádi; Gábor Wágner; Györg ..., Journal of Medicinal Chemistry, 2017

Negative allosteric modulators (NAM) of metabotropic glutamate receptor 5 (mGluR5) have been implicated as a potential pharmacotherapy for a number of psychiatric diseases, including anxiety and depression. Most of the mGluR5 NAM clinical candidates can be characterized by the central acetylenic ...


Combinatorial Strategy to Identify Fluorescent Probes for Biothiol and Thiophenol Based on Diversified Pyrimidine Moieties and Their Biological Applications

15-Feb-2017 | Xilei Xie; Mengmeng Li; Fuyan Tang; Yong Li; Leilei Zhang; Xiaoyun Jiao; Xu Wang; Bo Tang, Analytical Chemistry, 2017

We present a feasible paradigm of developing original fluorescent probes for target biomolecules via combinatorial chemistry. In this developmental program, pyrimidine moieties were investigated and optimized as unique recognition units for thiols for the first time through a parallel synthesis ...


Gram-scale Synthesis of a Novel Core Building Block for the New GPR40 Agonist Design

17-Nov-2016 | Lukin, Alexey; Bagnyukova, Daria; Zhurilo, Nikolay; Krasavin, Mikhail, Letters in Organic Chemistry, 2016

Abstract: Background: 3-[4-(Benzyloxy)phenyl]propanoic acid moiety is central to many advanced agonists of free fatty acid receptor 1 (FFA1 or GPR40) which are a new, promising class of antidiabetic drugs. An aldehydo carboxylic acid tert-butyl ester building block is required for speedy ...


A Trimethylsilylamine-Acyl Fluoride Amide Bond Forming Protocol for Weakly Nucleophilic Amines that is Amenable to the Parallel Synthesis of Di(hetero)arylamides

29-Sep-2016 | Maryam Zamiri; David S. Grierson, Synthesis, 2016

SynthesisDOI: 10.1055/s-0036-1588603 The reaction of a 2-pyridinone-based acid fluoride with the N–TMS derivatives of different weakly nucleophilic heteroaryl/arylamines in acetonitrile containing catalytic fluoride ion provides a clean, efficient and simple means to access a diverse range of ...


Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors

30-Aug-2016 | Mark Zak; Po-wai Yuen; Xiongcai Liu; Snahel Patel; Deepak Sampath; Jason Oeh; Bianca M. Liederer; Weiru Wang; Thomas ..., Journal of Medicinal Chemistry, 2016

NAMPT inhibitors may show potential as therapeutics for oncology. Throughout our NAMPT inhibitor program, we found that exposed pyridines or related heterocyclic systems in the left-hand portion of the inhibitors are necessary pharmacophores for potent cellular NAMPT inhibition. However, when ...


ChemInform Abstract: 2,2,2‐Trifluoroethyl Oxalates in the One‐Pot Parallel Synthesis of Hindered Aliphatic Oxamides.

18-Aug-2016 | Yurii S. Moroz, et al., ChemInform, 2016

Abstract Unsymmetrical N1,N2‐substituted aliphatic oxamides (52 examples) are prepared by stepwise aminolysis of methyl(trifluoroethyl)oxalate or bis(trifluoroethyl)oxalate with hindered primary and secondary aliphatic amines, resp., in moderate yields.


Synthesis of Benzothiophene‐Containing 10‐ and 11‐Membered Cyclic Phostones

13-Jul-2016 | Alexios N. Matralis, Youla S. Tsantrizos, European Journal of Organic Chemistry, 2016

Phosphinate and phosphonate derivatives can serve as useful transition‐state analogues of proteases, as substrate mimics of DNA/RNA‐processing enzymes, and as inhibitors of enzymes catalyzing the biosynthesis of isoprenoids. Synthetic methodologies for the preparation of medium‐sized ring ...


Sequence‐Defined Oligomers from Hydroxyproline Building Blocks for Parallel Synthesis Applications

01-Jul-2016 | Rosemary L. Kanasty, Arturo J. Vegas, Luke M. Ceo, Martin Maier, Klaus Charisse, Jayaprakash K. Nair, Robert Langer, ..., Angewandte Chemie International Edition, 2016

Abstract The functionality of natural biopolymers has inspired significant effort to develop sequence‐defined synthetic polymers for applications including molecular recognition, self‐assembly, and catalysis. Conjugation of synthetic materials to biomacromolecules has played an increasingly ...


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