当前位置： SCI文献检索 > ACS Combinatorial Science期刊下所有文献 > Polymer-supported stereoselective synthesis of tetrahydro-2H-oxazolo[3,2-a]pyrazin-5(3H)-ones from N-(2-oxo-ethyl)-derivatized dipeptides via eastbound iminiums.

Polymer-supported stereoselective synthesis of tetrahydro-2H-oxazolo[3,2-a]pyrazin-5(3H)-ones from N-(2-oxo-ethyl)-derivatized dipeptides via eastbound iminiums.

Abstract：

:Polymer-supported N-(2-oxo-ethyl)-derivatized Ser/Thr/Cys-containing dipeptides were synthesized and subjected to acid-mediated tandem N-acylium ion cyclization-nucleophilic addition to yield tetrahydro-2H-oxazolo[3,2-a]pyrazin-5(3H)-ones. The reaction conditions and building-block combinations for stereoselective synthesis of the newly formed asymmetric carbon were developed. The synthesis was fully compatible with solid-phase peptide synthesis, and the products serve as conformationally constrained peptidomimetics. The traceless synthesis of bicycles is also reported as part of this work.

journal_name

ACS Comb Sci

journal_title

ACS combinatorial science

authors

La Venia A,Dolenský B,Krchňák V

doi

10.1021/co3001567

subject

Has Abstract

pub_date

2013-03-11 00:00:00

pages

162-7

issue

3

eissn

2156-8952

issn

2156-8944

journal_volume

15

pub_type

杂志文章

相关文献

ACS Combinatorial Science文献大全
  • Screening Yeast Display Libraries against Magnetized Yeast Cell Targets Enables Efficient Isolation of Membrane Protein Binders.

    abstract：:When isolating binders from yeast displayed combinatorial libraries, a soluble, recombinantly expressed form of the target protein is typically utilized. As an alternative, we describe the use of target proteins displayed as surface fusions on magnetized yeast cells. In our strategy, the target protein is coexpressed ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00147

    authors： Bacon K,Burroughs M,Blain A,Menegatti S,Rao BM

    更新日期：2019-12-09 00:00:00

  • Exploring the First High-Entropy Thin Film Libraries: Composition Spread-Controlled Crystalline Structure.

    abstract：:Thin films of two types of high-entropy oxides (HEOs) have been deposited on 76.2 mm Si wafers using combinatorial sputter deposition. In one type of the oxides, (MgZnMnCoNi)O x , all the metals have a stable divalent oxidation state and similar cationic radii. In the second...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00159

    authors： Nguyen TX,Su YH,Hattrick-Simpers J,Joress H,Nagata T,Chang KS,Sarker S,Mehta A,Ting JM

    更新日期：2020-12-14 00:00:00

  • Copper-catalyzed multicomponent coupling/cycloisomerization reaction between substituted 1-formyl-9H-β-carbolines, secondary amines, and substituted alkynes for the synthesis of substituted 3-aminoindolizino[8,7-b]indoles.

    abstract：:A copper-catalyzed efficient one step three component strategy for preparing a library of aminoindolizino[8,7-b]indoles from N-substituted 1-formyl-9H-β-carbolines, secondary amines, and substituted alkynes with high atom economy has been developed. ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co300123y

    authors： Dighe SU,Hutait S,Batra S

    更新日期：2012-12-10 00:00:00

  • Combinatorial Investigations of High Temperature CuNb Oxide Phases for Photoelectrochemical Water Splitting.

    abstract：:High-throughput combinatorial methods have been useful in identifying new oxide semiconductors with the potential to be applied to solar water splitting. Most of these techniques have been limited to producing and screening oxide phases formed at temperatures below approximately 550 °C. We report the development of a ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00142

    authors： Skorupska K,Maggard PA,Eichberger R,Schwarzburg K,Shahbazi P,Zoellner B,Parkinson BA

    更新日期：2015-12-14 00:00:00

  • Acid-Promoted One-Pot Synthesis of Substituted Furan and 6-Methylpyrazin-2(1 H)-one Derivatives via Allene Intermediate Formed in Situ.

    abstract：:Under the acidic conditions, substituted furans were constructed from γ-alkynyl ketones through corresponding allene intermediates in one-pot. The methodology was also tailored to a series of the Ugi reaction products for the synthesis of 6-methylpyrazin-2(1 H)-one derivatives. The current method offered significant a...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.8b00005

    authors： Lei J,Xu ZG,Tang DY,Li Y,Xu J,Li HY,Zhu J,Chen ZZ

    更新日期：2018-05-14 00:00:00

  • Telescoped Synthesis of 2-Acyl-1-aryl-1,2-dihydroisoquinolines and Their Inhibition of the Transcription Factor NF-κB.

    abstract：:A sequential single-flask multicomponent reactions is highly effective for the synthesis of 1,2-dihydroisoquinolines through amidealkylation from intermediate N-acylisoquinolinium salts under mild conditions. N-Acylisoquinolinium ions and trichloromethyl-1-(1H-indol-3-yl)isoquinoline-2(1H)-carboxylate have demonstrate...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00001

    authors： Chung TW,Hung YT,Thikekar T,Paike VV,Lo FY,Tsai PH,Liang MC,Sun CM

    更新日期：2015-08-10 00:00:00

  • Magnetic Bead-Immobilized Mammalian Cells Are Effective Targets to Enrich Ligand-Displaying Yeast.

    abstract：:Yeast surface display empowers selection of protein binding ligands, typically using recombinant soluble antigens. However, ectodomain fragments of transmembrane targets may fail to recapitulate their true, membrane-bound form. Direct selections against adhered mammalian cells empower enrichment of genuine binders yet...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00036

    authors： Lown PS,Hackel BJ

    更新日期：2020-05-11 00:00:00

  • One-pot sequential alkynylation and cycloaddition: regioselective construction and biological evaluation of novel benzoxazole-triazole derivatives.

    abstract：:Individually, benzoxazole and triazole moieties are of significant biological interest owing to their importance in drugs and pharmaceuticals. To assess their combined biological impact when woven into one molecule, we designed a novel, regioselective, multicomponent, one-pot (MCOP) approach for the construction of be...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co500135z

    authors： Srivastava A,Aggarwal L,Jain N

    更新日期：2015-01-12 00:00:00

  • (Hetero-)(arylidene)arylhydrazides as Multitarget-Directed Monoamine Oxidase Inhibitors.

    abstract：:Fourteen (hetero-)(arylidene)arylhydrazide derivatives (ABH1-ABH14) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound ABH5 most potently inhibited MAO-B with an IC50 value of 0.025 ± 0.0019 μM; ABH2 and ABH3 exhibited high IC50 ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00136

    authors： Palakkathondi A,Oh JM,Dev S,Rangarajan TM,Kaipakasseri S,Kavully FS,Gambacorta N,Nicolotti O,Kim H,Mathew B

    更新日期：2020-11-09 00:00:00

  • Application of Silica-Supported Alkylating Reagents in a One-Pot, Sequential Protocol to Diverse Benzoxathiazepine 1,1-Dioxides.

    abstract：:Applications of silica-ROMP reagents in a one-pot, sequential protocol have been developed for the synthesis of a variety of diverse benzoxathiazepine 1,1-dioxides. This protocol includes sulfonylation, intramolecular SNAr, alkylation with silica-supported oligomeric benzyl (Si-OBPn) and triazole (Si-OTPn) phosphates,...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.6b00041

    authors： Faisal S,Maity PK,Zang Q,Samarakoon TB,Sourk RL,Hanson PR

    更新日期：2016-07-11 00:00:00

  • Structural and Functional Properties of the Thin Film System Ti-Ni-Si.

    abstract：:The thin film system Ti-Ni-Si was investigated using methods of combinatorial materials science. A thin film composition spread library of the system was fabricated using combinatorial magnetron sputtering. The functional properties Seebeck coefficient, electrical resistivity, and luminance were determined using high-...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.8b00181

    authors： Wambach M,Ziolkowski P,Müller E,Ludwig A

    更新日期：2019-05-13 00:00:00

  • Application of High-Throughput Seebeck Microprobe Measurements on Thermoelectric Half-Heusler Thin Film Combinatorial Material Libraries.

    abstract：:In view of the variety and complexity of thermoelectric (TE) material systems, combinatorial approaches to materials development come to the fore for identifying new promising compounds. The success of this approach is related to the availability and reliability of high-throughput characterization methods for identify...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.7b00019

    authors： Ziolkowski P,Wambach M,Ludwig A,Mueller E

    更新日期：2018-01-08 00:00:00

  • One-pot, three-component reaction using modified Julia reagents: a facile synthesis of 4,5-disubstituted 1,2,3-(NH)-triazoles in a wet organic solvent.

    abstract：:A new one-pot, three component reaction involving the use of Julia reagent, aldehyde, and sodium azide was developed for the efficient synthesis of N-unsubstituted 1,2,3-triazoles. This reaction could be carried out under mild reaction conditions without any precaution, and broad scope of substrates, both respect to J...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co5001597

    authors： Chai H,Guo R,Yin W,Cheng L,Liu R,Chu C

    更新日期：2015-03-09 00:00:00

  • First-Principles Computational Screening of Perovskite Hydrides for Hydrogen Release.

    abstract：:This study investigates perovskite hydrides (ABH3) comprising alkali metals of A, where A is Li, Na, K, Rb, or Cs, and alkaline-earth metals of B, where B is Be, Mg, Ca, Sr, or Ba, to screen the highest potential hydrides for hydrogen release. Herein, we investigated the most favorable dehydrogenation pathway for each...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00108

    authors： Li Y,Chung JS,Kang SG

    更新日期：2019-11-11 00:00:00

  • Solid-supported cross-metathesis and a formal alkane metathesis for the generation of biologically relevant molecules.

    abstract：:Solid-phase synthetic strategies toward the generation of libraries of biologically relevant molecules were developed using olefin cross-metathesis as a key step. It is remarkably the formal alkane metathesis based on a one-pot, microwave-assisted, ruthenium-catalyzed cross-metathesis and reduction to obtain Csp3-Csp3...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co500176b

    authors： Méndez L,Mata EG

    更新日期：2015-02-09 00:00:00

  • Mapping Structure-Composition-Property Relationships in V- and Fe-Doped LiMnPO4 Cathodes for Lithium-Ion Batteries.

    abstract：:A series of LiMn1-x-yFexVyPO4 (LMFVP) nanomaterials have been synthesized using a pilot-scale continuous hydrothermal synthesis process (CHFS) and evaluated as high voltage cathodes in Li-ion batteries at a production rate of 0.25 kg h-1. The rapid synthesis and screening approach has allowed the specific capacity of ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.6b00035

    authors： Johnson ID,Loveridge M,Bhagat R,Darr JA

    更新日期：2016-11-14 00:00:00

  • Optimization of Criteria for an Efficient Screening of New Thermoelectric Compounds: The TiNiSi Structure-Type as a Case-Study.

    abstract：:High-throughput calculations can be applied to a large number of compounds, in order to discover new useful materials. In the present work, ternary intermetallic compounds are investigated, to find new potentially interesting materials for thermoelectric applications. The screening of stable nonmetallic compounds requ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00133

    authors： Barreteau C,Crivello JC,Joubert JM,Alleno E

    更新日期：2020-12-14 00:00:00

  • Combinatorial screening of potentiometric Pb(II) sensors from polysulfoaminoanthraquinone solid ionophore.

    abstract：:A potentiometric Pb(II)-selective sensor was fabricated by a combinatorial screening of electrically conducting polysulfoaminoanthraquinone (PSA) nanoparticles as a solid ionophore, ion exchangers (oleic acid (OA) and NaTPB), plasticizers in a polyvinyl chloride (PVC) matrix, membrane thickness, inner filling ion spec...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co400140g

    authors： Huang MR,Ding YB,Li XG

    更新日期：2014-03-10 00:00:00

  • Solid-Phase Synthesis of Oligopeptides Containing Sterically Hindered Amino Acids on Nonswellable Resin Using 3-Nitro-1,2,4-triazol-1-yl-tris(pyrrolidin-1-yl)phosphonium Hexafluorophosphate (PyNTP) as the Condensing Reagent.

    abstract：:Peptides are still difficult to synthesize when they contain sterically hindered amino acids, such as α,α-disubstituted amino acids and N-substituted amino acids. In this study, solid-phase syntheses of oligopeptides containing multiple α-aminoisobutyric acid (Aib) residues were performed in high yields by using a non...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.7b00184

    authors： Hara RI,Mitsuhashi Y,Saito K,Maeda Y,Wada T

    更新日期：2018-03-12 00:00:00

  • Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.

    abstract：:Protein-protein interactions are generally challenging to target by small molecules. To address the challenge, we have used a multidisciplinary approach to identify small-molecule disruptors of protein-protein interactions that are mediated by SUMO (small ubiquitin-like modifier) proteins. SUMO modifications have emer...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co500181b

    authors： Alontaga AY,Li Y,Chen CH,Ma CT,Malany S,Key DE,Sergienko E,Sun Q,Whipple DA,Matharu DS,Li B,Vega R,Li YJ,Schoenen FJ,Blagg BS,Chung TD,Chen Y

    更新日期：2015-04-13 00:00:00

  • Semiautomated Parallel RAFT Copolymerization of Isoprene with Glycidyl Methacrylate.

    abstract：:Copolymerization of isoprene (IP) with glycidyl methacrylate (GMA) was performed under RAFT (reversible addition-fragmentation chain-transfer) polymerization conditions in a platform for high-output experimentation. Covering the range between 1 and 0.2 molar fraction of IP in the feed, four sets of reactions were carr...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00110

    authors： Rosales-Guzmán M,Pérez-Camacho O,Guerrero-Sánchez C,Harrisson S,Torres-Lubián R,Vitz J,Schubert US,Saldívar-Guerra E

    更新日期：2019-12-09 00:00:00

  • An Integrated Microfluidic Processor for DNA-Encoded Combinatorial Library Functional Screening.

    abstract：:DNA-encoded synthesis is rekindling interest in combinatorial compound libraries for drug discovery and in technology for automated and quantitative library screening. Here, we disclose a microfluidic circuit that enables functional screens of DNA-encoded compound beads. The device carries out library bead distributio...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.6b00192

    authors： MacConnell AB,Price AK,Paegel BM

    更新日期：2017-03-13 00:00:00

  • Development of Measurement Tools for High-Throughput Experiments of Synchrotron Radiation XRD and XAFS on Powder Libraries.

    abstract：:We propose to minimize the sampling time for high-throughput measurements of powder X-ray diffraction (XRD) and X-ray absorption fine structure (XAFS) in synchrotron radiation. The conventional synchrotron radiation powder X-ray diffraction method requires filling of a capillary tube, but a structure-refining diffract...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00174

    authors： Fujimoto K,Aimi A,Maruyama S

    更新日期：2020-12-14 00:00:00

  • Development of High-Throughput Methods for Sodium-Ion Battery Cathodes.

    abstract：:Combinatorial synthesis of Li-ion batteries has proven extremely powerful in screening complex compositional spaces for next-generation materials. To date, no Na-ion counterpart exists wherein Na-ion cathodes can be synthesized in such a way to be comparable to that obtained in bulk synthesis. Herein, we develop a syn...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00181

    authors： Adhikari T,Hebert A,Adamič M,Yao J,Potts K,McCalla E

    更新日期：2020-06-08 00:00:00

  • Evaluation of the Two-Dimensional Performances of Low Activity Planar Catalysts: Development and Validation of a True Scanning Reactor.

    abstract：:The development of a scanning reactor for planar catalysts is presented here. With respect to other existing models, this reactor is able to scan catalysts even with low turnover frequencies with a minimum sensed circular area of approximately 6 mm in diameter. The downstream gas analysis is performed with a quaprupol...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00103

    authors： Marelli M,Nemenyi A,Dal Santo V,Psaro R,Ostinelli L,Monticelli D,Dossi C,Recchia S

    更新日期：2016-01-11 00:00:00

  • Parallel synthesis of a desketoraloxifene analogue library via iodocyclization/palladium-catalyzed coupling.

    abstract：:For a future structure-activity relationship (SAR) study, a library of desketoraloxifene analogues has been prepared by parallel synthesis using iodocyclization and subsequent palladium-catalyzed coupling reactions. Points of desketoraloxifene diversification involve the two phenolic hydroxyl groups and the aliphatic ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co200090p

    authors： Cho CH,Jung DI,Neuenswander B,Larock RC

    更新日期：2011-09-12 00:00:00

  • Effects of the Ion to Growth Flux Ratio on the Constitution and Mechanical Properties of Cr1-x-Alx-N Thin Films.

    abstract：:Cr-Al-N thin film materials libraries were synthesized by combinatorial reactive high power impulse magnetron sputtering (HiPIMS). Different HiPIMS repetition frequencies and peak power densities were applied altering the ion to growth flux ratio. Moreover, time-resolved ion energy distribution functions were measured...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00123

    authors： Banko L,Ries S,Grochla D,Arghavani M,Salomon S,Pfetzing-Micklich J,Kostka A,Rogalla D,Schulze J,Awakowicz P,Ludwig A

    更新日期：2019-12-09 00:00:00

  • A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts.

    abstract：:A set of chemically engineered extracts enriched in compounds including N-N and N-O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one oxime hit that interacts with TcBDF3 with affinity in the submicromolar range and that shows interes...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.7b00172

    authors： Ramallo IA,Alonso VL,Rua F,Serra E,Furlan RLE

    更新日期：2018-04-09 00:00:00

  • A Novel pseudo-Four-Component Domino Reaction for the Synthesis of Naphtho[2,1-b]furan-2(1H)-ones Using a Nanocatalyst.

    abstract：:In this article, an original one-pot method is utilized to synthesize a variety of derivatives of naphtho[2,1-b]furan-2(1H)-one via a pseudo-four-component domino reaction of aryl aldehydes, acetic anhydride, hippuric acids, and 2-naphthols catalyzed by HSW@SPIONs. This reaction illustrates an array of attractive feat...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00018

    authors： Salami-Ranjbaran E,Khosropour AR,Mohammadpoor-Baltork I,Moghadam M,Tangestaninejad S,Mirkhani V

    更新日期：2015-08-10 00:00:00

  • Diversity-oriented synthesis of spiro-substituted 1,3-thiazine library via a one-pot, two-step, three-component reaction.

    abstract：:A sequential one-pot, two-step, three-component reaction for efficient synthesis of spiro-substituted 1,3-thiazine library has been developed. The syntheses were achieved by reacting cyanoacetamide with isothiocyanate derivatives to give rise to 2-cyano-3-mercaptoacrylamides, which are trapped in situ by various cyclo...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co100034v

    authors： Zhuang QY,Wang X,Gao Y,Shi F,Jiang B,Tu SJ

    更新日期：2011-01-10 00:00:00