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：: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

authors： Kanchithalaivan S,Sumesh RV,Kumar RR

更新日期：2014-10-13 00:00:00

abstract：:Solid-phase synthesis is the method of choice for peptide preparation in both research and industrial settings. The whole synthetic process is governed by the initial functionalization of the resin. Although the literature provides several methods to determine such functionalization, the addition of an Fmoc-amino acid...

journal_title：ACS combinatorial science

authors： Al Musaimi O,Basso A,de la Torre BG,Albericio F

更新日期：2019-11-11 00:00:00

abstract：:A combinatorial library having 66 different ternary compositions of Pd-Ir-Ce was prepared via the impregnation method to find the optimum ternary composition with the highest performance toward oxygen reduction reaction (ORR) in acid media. Its performance in ORR activity of the combinatorial array was evaluated throu...

journal_title：ACS combinatorial science

authors： Park SH,Choi CH,Koh JK,Pak C,Jin SA,Woo SI

更新日期：2013-11-11 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

authors： Xie YJ,Sun J,Yan CG

更新日期：2014-06-09 00:00:00

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

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

更新日期：2011-09-12 00:00:00

abstract：:A novel and highly efficient three-component reaction of 2-alkynylbenzaldoxime, carbodiimide, with electrophile (bromine or iodine monochloride) is disclosed, which generates 1-(4-haloisoquinolin-1-yl)ureas in good yields under mild conditions. Subsequent palladium-catalyzed Suzuki-Miyaura coupling reaction is introdu...

journal_title：ACS combinatorial science

authors： Ye S,Wang H,Wu J

更新日期：2011-03-14 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

authors： MacConnell AB,Price AK,Paegel BM

更新日期：2017-03-13 00:00:00

abstract：:Preparative RP-LCMS is widely used to purify compounds from crude reaction mixtures in drug discovery today. Method development for preparative Liquid Chromatography-Mass Spectrometry (LCMS) consists of finding the right balance between speed and quality, often leading to the use of fast generic gradients (5-95% organ...

journal_title：ACS combinatorial science

authors： Koza P,Gonnot V,Pelleter J

更新日期：2012-04-09 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

authors： Chen YY,Chang LT,Chen HW,Yang CY,Hsin LW

更新日期：2017-03-13 00:00:00

abstract：:Functionalized chromenes have been synthesized via highly selective metal-free domino reactions from ketones and phenols. 2H-Chromenes, 4H-chromenes, spiran and benzocyclopentane can be respectively prepared starting from the corresponding cyclic ketones, aryl methyl ketones, acetone, and 3-pentanone. ...

journal_title：ACS combinatorial science

authors： Xue WJ,Li Q,Gao FF,Zhu YP,Wang JG,Zhang W,Wu AX

更新日期：2012-08-13 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

authors： Fernandez M,Abreu JI,Shi H,Barnard AS

更新日期：2016-11-14 00:00:00

abstract：:An efficient and straightforward synthetic protocol has been developed for the diversity-oriented synthesis of highly functionalized piperidines containing a Meldrum's acid moiety via pseudo five-component reaction between aromatic aldehydes, ammonium acetate, substituted β-nitrostyrenes and Meldrum's acid for the gen...

journal_title：ACS combinatorial science

authors： Li Y,Xue Z,Ye W,Liu J,Yao J,Wang C

更新日期：2014-03-10 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

authors： Maier WF

更新日期：2019-06-10 00:00:00

abstract：:Disulfide exchange screening is a method for evaluating the binding of small molecule fragments to proteins that have at least one accessible cysteine. While operationally simple, it does require a large library of small fragment molecules bearing disulfide-containing side chains. These specialized fragments are not a...

journal_title：ACS combinatorial science

authors： Burlingame MA,Tom CT,Renslo AR

更新日期：2011-05-09 00:00:00

abstract：:A microgradient-heater (MGH) was developed, and its feasibility as a tool for high-throughput materials science experimentation was tested. The MGH is derived from microhot plate (MHP) systems and allows combinatorial thermal processing on the micronano scale. The temperature gradient is adjustable by the substrate ma...

journal_title：ACS combinatorial science

authors： Meyer R,Hamann S,Ehmann M,Thienhaus S,Jaeger S,Thiede T,Devi A,Fischer RA,Ludwig A

更新日期：2012-10-08 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

authors： Méndez L,Mata EG

更新日期：2015-02-09 00:00:00

abstract：:An efficient method is described for the solid-supported synthesis of imidazo[4,5-b]pyridines and imidazo[4,5-c]pyridines from 2,4-dichloro-3-nitropyridine. The key pyridine building block was reacted with polymer-supported amines, followed by replacement of the second chlorine with amines, nitro group reduction, and ...

journal_title：ACS combinatorial science

authors： Lemrová B,Smyslová P,Popa I,Oždian T,Zajdel P,Soural M

更新日期：2014-10-13 00:00:00

abstract：:A build/couple/pair strategy for the synthesis of complex and densely functionalized small molecules is presented. The strategy relies on synthetically tractable building blocks (build), that is, diversely substituted hydrazides, α-hydroxy aldehydes, and boronic acids, which undergo Petasis 3-component reactions (coup...

journal_title：ACS combinatorial science

authors： Flagstad T,Hansen MR,Le Quement ST,Givskov M,Nielsen TE

更新日期：2015-01-12 00:00:00

abstract：:A novel three-component, two-step, one-pot nucleophilic aromatic substitution (SNAr)-intramolecular cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin analogs was synth...

journal_title：ACS combinatorial science

authors： Li H,Sun W,Huang X,Lu X,Patel PR,Kim M,Orr MJ,Fisher RM,Tanaka TQ,McKew JC,Simeonov A,Sanderson PE,Zheng W,Williamson KC,Huang W

更新日期：2017-12-11 00:00:00

abstract：:Magnetization using cheap and minimally toxic materials, such as iron oxide nanoparticles can enable easy separation of cells from culture medium and is relevant to several industrial applications. Here, we show that cell surface expression of a mutant protein that binds iron oxide can enable efficient magnetization o...

journal_title：ACS combinatorial science

authors： Cruz-Teran CA,Bacon K,McArthur N,Rao BM

更新日期：2018-10-08 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

authors： Huang MR,Ding YB,Li XG

更新日期：2014-03-10 00:00:00

abstract：:3-Substituted 4-quinolones were synthesized using a one-pot metal-free strategy in moderate to quantitative yields. Carried out in dimethylsulfoxide (DMSO) via a sequential addition of materials, the methodology is tolerant of a wide range of functional groups and applicable to library synthesis. ...

journal_title：ACS combinatorial science

authors： Liu QL,Li QL,Fei XD,Zhu YM

更新日期：2011-01-10 00:00:00

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

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

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

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

更新日期：2016-07-11 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

authors： Baumann M,Baxendale IR,Kuratli C,Ley SV,Martin RE,Schneider J

更新日期：2011-07-11 00:00:00

abstract：:Parallel solution-phase synthesis of combinatorial libraries of dihydroindenoisoquinolines employing a sequential Cu(I)/Pd(0)-catalyzed multicomponent coupling and annulation protocol was realized. The scope and limitations of the protocol with respect to the substitution pattern in the aryl ring of the indene core, a...

journal_title：ACS combinatorial science

authors： Kumar S,Painter TO,Pal BK,Neuenswander B,Malinakova HC

更新日期：2011-09-12 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

authors： Suram SK,Newhouse PF,Gregoire JM

更新日期：2016-11-14 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

authors： Newhouse PF,Zhou L,Umehara M,Boyd DA,Soedarmadji E,Haber JA,Gregoire JM

更新日期：2020-12-14 00:00:00

abstract：:A three-component reaction of a 2-aminoazine, a 2-oxoaldehyde, and a cyclic 1,3-dicarbonyl compound providing access toward a novel class of imidazo[1,2-a]azine derivatives was developed and studied. The scope of the process was thoroughly explored under three different reaction conditions resulting in the generation ...

journal_title：ACS combinatorial science

authors： Peshkov VA,Peshkov AA,Pereshivko OP,Van Hecke K,Zamigaylo LL,Van der Eycken EV,Gorobets NY

更新日期：2014-10-13 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

authors： Postma TM,Albericio F

更新日期：2014-04-14 00:00:00