Abstract:
:A one-pot parallel synthesis of N(1)-aryl-N(2)-alkyl-substituted oxamides with 2,2,2-trifluoroethyl chlorooxoacetate was developed. The synthesis of a library of 45 oxamides revealed higher efficiency of this reagent over the known ethyl chlorooxoacetate. The reagent was successfully used to prepare the known oxamide-containing HIV entry inhibitors.
journal_name
ACS Comb Scijournal_title
ACS combinatorial scienceauthors
Bogolubsky AV,Moroz YS,Mykhailiuk PK,Pipko SE,Zhemera AV,Konovets AI,Stepaniuk OO,Myronchuk IS,Dmytriv YV,Doroschuk RA,Zaporozhets OA,Tolmachev Adoi
10.1021/acscombsci.5b00091subject
Has Abstractpub_date
2015-10-12 00:00:00pages
615-22issue
10eissn
2156-8952issn
2156-8944journal_volume
17pub_type
杂志文章abstract::We have implemented an aldol-based "build/couple/pair" (B/C/P) strategy for the synthesis of stereochemically diverse 8-membered lactam and sultam scaffolds via S(N)Ar cycloetherification. Each scaffold contains two handles, an amine and aryl bromide, for solid-phase diversification via N-capping and Pd-mediated cross...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co2000218
更新日期:2011-07-11 00:00:00
abstract::High-throughput experimentation provides efficient mapping of composition-property relationships, and its implementation for the discovery of optical materials enables advancements in solar energy and other technologies. In a high throughput pipeline, automated data processing algorithms are often required to match ex...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00053
更新日期:2016-11-14 00:00:00
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
更新日期:2011-01-10 00:00:00
abstract::A fast and facile synthesis of a series of 4-nitrophenyl 2-azidoethylcarbamate derivatives as activated urea building blocks was developed. The N-Fmoc-protected 2-aminoethyl mesylates derived from various commercially available N-Fmoc-protected α-amino acids, including those having functionalized side chains with acid...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00160
更新日期:2017-03-13 00:00:00
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
更新日期:2019-05-13 00:00:00
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
更新日期:2015-02-09 00:00:00
abstract::This paper describes the synthesis of a 300 member library of 3,5-substituted enones. The synthesis starts with 6 different bromoenones that are accessed from the corresponding 1,3 diones. These bromides are then diversified by Suzuki coupling with a variety of aromatic and vinyl boronic acids. Additionally a small se...
journal_title:ACS combinatorial science
pub_type: 信件
doi:10.1021/co200070m
更新日期:2011-07-11 00:00:00
abstract::This is a report on the early years of combinatorial materials science and technology. High-throughput technologies (HTTs) are found in life- and materials-science laboratories. Although HTTs have long been the standard in life sciences in academia as well as in industry, HTTs in materials science have become the stan...
journal_title:ACS combinatorial science
pub_type: 历史文章,杂志文章,评审
doi:10.1021/acscombsci.8b00189
更新日期:2019-06-10 00:00:00
abstract::A novel immobilized N-chlorosuccinimide resin was developed for peptide disulfide bond formation in combinatorial libraries. The resin is prepared in a simple two-step process from commercial starting materials. Disulfide formation is initiated by adding a peptide solution to the resin, and excess reagent is removed b...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500003p
更新日期:2014-04-14 00:00:00
abstract::We report the parallel synthesis of a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-3-ium chloride salts, which are analogs to cationic anthraquinones. Three synthetic protocols were examined leading to a convenient and facile library synthesis of the cationic anthraquinone analogs that contain...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co2002075
更新日期:2012-03-12 00:00:00
abstract::The possibility of band gap engineering in graphene opens countless new opportunities for application in nanoelectronics. In this work, the energy gaps of 622 computationally optimized graphene nanoflakes were mapped to topological autocorrelation vectors using machine learning techniques. Machine learning modeling re...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00094
更新日期:2016-11-14 00:00:00
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
更新日期:2012-12-10 00:00:00
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
更新日期:2014-03-10 00:00:00
abstract::A combination of flow and batch chemistries has been successfully applied to the assembly of a series of trisubstituted drug-like pyrrolidines. This study demonstrates the efficient preparation of a focused library of these pharmaceutically important structures using microreactor technologies, as well as classical par...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co2000357
更新日期:2011-07-11 00:00:00
abstract::The diversity oriented synthesis of substituted pyridines and dihydro-6H-quinolin-5-ones tethered with aryls and heteroaryls was achieved in very good yields through CeCl(3)·7H(2)O-NaI catalyst via variants of the Bohlmann-Rahtz reaction. β-Enaminones derived from various aryl and heteroaryl methyl ketones were regios...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co2000604
更新日期:2011-07-11 00:00:00
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
更新日期:2020-12-14 00:00:00
abstract::Retinoic acid (RA) is a key metabolite necessary for embryonic development and differentiation in vertebrates. We demonstrate the utility of genetically encoded, ligand-activatable single-chain bioluminescence probes for detecting RAs from different biological sources. We examined 13 different molecular designs to ide...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.9b00035
更新日期:2019-06-10 00:00:00
abstract::Ultrasound-assisted synthesis of benzimidazo[2,1-b]quinazolin-1(1H)-ones was achieved via piperidine-catalyzed three-component reaction of 2-aminobenzimidazoles, an aromatic aldehyde, and 1,3-dione in aqueous isopropanol. This mechanism was first suspected following our identification of unusual reaction intermediates...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00186
更新日期:2016-03-14 00:00:00
abstract::The present investigation reports an easy access to a library of novel spiro-oxindole-pyrrolizine or pyrrolo[1,2-c]thiazole fused coumarin hybrid heterocycles through a one-pot sequential four-component reactions of 2,2-dimethyl-1,3-dioxane-4,6-dione, salicylaldehydes, isatins, and cyclic α-amino acids under ultrasoun...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500092b
更新日期:2014-10-13 00:00:00
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
更新日期:2020-12-14 00:00:00
abstract::A condition-based skeletal divergent synthesis was explored to achieve skeletal diversity in two component condensation reaction. Cyanomethyl benzimidazole was reacted with α-bromoketone under thermal conditions to furnish 2-aminofuranyl-benzimidazoles, while the same reaction afforded 3-cyano-benzopyrrolo-imidazoles ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.7b00052
更新日期:2017-07-10 00:00:00
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 syn...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co3001567
更新日期:2013-03-11 00:00:00
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
更新日期:2017-03-13 00:00:00
abstract::An unprecedented three-component C(sp(3))-H functionalization of 2-alkylazaarenes with aryl aldehydes and 4-hydroxycoumarins was realized, providing azaarene-substituted 3-benzyl-4-hydroxycoumarins in good to excellent yields. These new target compounds displayed broad-spectrum antibacterial activities, providing a ne...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00082
更新日期:2016-09-12 00:00:00
abstract::A high throughput combinatorial synthesis utilizing inkjet printing of precursor inks was used to rapidly evaluate Bi-alloying into double perovskite oxides for enhanced visible light absorption. The fast visual screening of photo image scans of the library plates identifies 4-metal oxide compositions displaying an in...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.0c00177
更新日期:2020-12-14 00:00:00
abstract::The reactions of vinyl malononitriles with 3-phenacylideneoxindoles in ethanol in the presence of DBU as base resulted in the functionalized spirocyclic oxindoles through the domino Michael addition and intramolecular nucleophilic addition to cyano group. On the other hand, the similar reaction in the presence of pipe...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500006c
更新日期:2014-06-09 00:00:00
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
更新日期:2015-04-13 00:00:00
abstract::Acetylenic tertiary alcohols are well-known to be compounds that are biologically more stable than their corresponding secondary alcohols. The linkage of an acetylenic compound to a polymer support and further introduction of molecular diversity was found to be an interesting way to generate libraries of hydroxy acety...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co300034y
更新日期:2012-06-11 00:00:00
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
更新日期:2020-11-09 00:00:00
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
更新日期:2016-07-11 00:00:00