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Journal of Combinatorial Chemistry

Roland E Dolle, Bertrand Le Bourdonnec, Karin Worm, Guillermo A Morales, Craig J Thomas, Wei Zhang
No abstract text is available yet for this article.
November 8, 2010: Journal of Combinatorial Chemistry
Harold N Weller, Katalin Ebinger, William Bullock, Kurt J Edinger, Mark A Hermsmeier, Steven L Hoffman, David S Nirschl, Thomas Swann, Jiang Zhao, Jeffrey Kiplinger, Paul Lefebvre
Preparative HPLC and HPLC-MS are well established as the methods of choice for purification of pharmaceutical library compounds. Recent advances in supercritical fluid chromatography (SFC) have now made SFC a viable alternative to HPLC for this application. One of the potential arguments for using SFC in place of, or in addition to, HPLC is that it may offer different selectivity and thus has the potential for improved separation success rates. In this paper, we examine relative success rates for SFC and HPLC in obtaining adequate selectivity for successful separation...
November 8, 2010: Journal of Combinatorial Chemistry
Dengfeng Dou, Prasanth Viwanathan, Yi Li, Guijia He, Kevin R Alliston, Gerald H Lushington, Joshua D Brown-Clay, R Padmanabhan, William C Groutas
The 1-oxo-1, 2, 3, 4-tetrahydroisoquinoline and 1-Oxo-1, 2-dihydroisoquinoline scaffolds were utilized in the design and solution phase synthesis of focused libraries of compounds for screening against West Nile Virus (WNV) protease. Exploratory studies have led to the identification of a WNV protease inhibitor (a 1-oxo-1, 2-dihydroisoquinoline-based derivative, 12j) which could potentially serve as a launching pad for a hit-to-lead optimization campaign. The identified hit was devoid of any inhibitory activity toward a panel of mammalian serine proteases...
November 8, 2010: Journal of Combinatorial Chemistry
Simon Maechling, James Good, Stephen D Lindell
No abstract text is available yet for this article.
November 8, 2010: Journal of Combinatorial Chemistry
Alan Rolfe, Thiwanka B Samarakoon, Sarra V Klimberg, Marek Brzozowski, Benjamin Neuenswander, Gerald H Lushington, Paul R Hanson
The construction of a library of benzothiaoxazepine-1,1'-dioxides utilizing a one-pot, S(N)Ar diversification-ODCT(50) scavenging protocol is reported. This protocol combines microwave irradiation to facilitate the reaction, in conjunction with a soluble ROMP-derived scavenger (ODCT) to afford the desired products in good overall purity. Utilizing this protocol, a 78-member library was successfully synthesized and submitted for biological evaluation.
November 8, 2010: Journal of Combinatorial Chemistry
Natalia E Monge, María C Miras, César A Barbero
No abstract text is available yet for this article.
November 8, 2010: Journal of Combinatorial Chemistry
Dhevalapally B Ramachary, Kinthada Ramakumar, Adluri Bharanishashank, Vidadala V Narayana
A general, sustainable and practical process for the sequential cascade one-pot synthesis of library of highly substituted push-pull olefins, phenols and 2-methyl-2H-chromenes was reported through multicatalysis cascade (MCC) reactions. Direct sequential one-pot combination of amine- or amino acid-catalyzed cascade Knoevenagel/Michael/aldol condensation/decarboxylation with other reactions like amine- or amino acid-catalyzed cascade Claisen-Schmidt/iso-aromatization, Claisen-Schmidt/isomerization, Claisen-Schmidt/iso-aromatization/isomerization, Michael addition, Claisen-Schmidt/Michael, ruthenium-base-silica-catalyzed ring closing metathesis/base-induced ring-opening/benzylic oxidation/[1,7]-sigmatropic hydrogen shift, or ruthenium-base-heat-catalyzed ring closing metathesis/base-induced ring-opening/[1,7]-sigmatropic hydrogen shift reactions of alkyl acetoacetates, a variety of aldehydes and alkyl halides furnished the highly functionalized push-pull olefins, phenols and 2-methyl-2H-chromenes with high yields...
November 8, 2010: Journal of Combinatorial Chemistry
Yichuan Liao, Huayao Li, Yuan Liu, Zhijun Zou, Dawen Zeng, Changsheng Xie
On the basis of combinatorial methodology and the idea of an equilateral ingredient triangle, the TiO(2)/ZnO/Fe(2)O(3) composite system including 66 ingredient points was designed. The photocurrents under different light sources and bias voltages were measured, and the photocurrent amplitude at 300 s was chosen as a parameter to evaluate the photoelectric response of the composite. To appraise the composition effect of the composite compared with pure materials, the quantitative formula of the composition effect has been provided for the first time in this paper...
November 8, 2010: Journal of Combinatorial Chemistry
Barbora Vanková, Jan Hlavác, Miroslav Soural
Solid-phase synthesis of bisheterocyclic compounds that contain purine and the 3-hydroxyquinolin-4(1H)-one skeleton connected with an aliphatic spacer of a different length/structure is described. The reaction sequence started from the primary amines immobilized on aminomethylated polystyrene resin equipped with an acid-labile linker (4-(4-formyl-3-methoxyphenoxy)butyric acid). After the arylation of amines with 2,6-dichloropurine via its C(6), purine N(9) was alkylated and subsequently the chlorine at purine C(2) was substituted with aliphatic diamines...
November 8, 2010: Journal of Combinatorial Chemistry
Dewen Li, Shudong Duan, Youhong Hu
A novel benzopyrano[4,3-d]pyrimidine scaffold was generated via a three-component one-pot reaction from iodochromone, alkyne, and an amidine through a Sonogashira coupling, condensation, and cycloaddition. This combinatorial synthetic approach provides an efficient, easy construction of a diversified heterocyclic compounds library.
November 8, 2010: Journal of Combinatorial Chemistry
Alireza Hasaninejad, Abdolkarim Zare, Mohsen Shekouhy, Javad Ameri Rad
A catalyst-free one-pot four component methodology for the synthesis of 1,2,4,5-substituted imidazoles under conventional heating and microwave irradiation using 1-butyl-3-methylimidazolium bromide, [Bmim]Br, as a neutral reaction media is described. A broad range of structurally diverse aldehydes (aromatic aldehydes bearing electron withdrawing and/or electron releasing groups as well as heteroaromatic aldehydes) and primary amines (aromatic and aliphatic) were applied successfully, and corresponding products were obtained in good to excellent yields without any byproduct...
November 8, 2010: Journal of Combinatorial Chemistry
Xiao-Jin Wu, Ran Jiang, Xiao-Ping Xu, Xiao-Ming Su, Wei-Hong Lu, Shun-Jun Ji
A convenient and highly efficient multicomponent protocol has been developed for the synthesis of various poly-substituted 2-(pyridin-2-yl)imidazoles from 2-cyanopyridine, corresponding aromatic aldehydes, and NH(4)OAc/primary amine. Notably, tri-substituted 2-(pyridin-2-yl)imidazoles were highly yielded when aromatic primary amines were used as substrates, but both di- and tri-substituted 2-(pyridin-2-yl)imidazoles were obtained in one pot when some aliphatic primary amines were used as substrates.
November 8, 2010: Journal of Combinatorial Chemistry
Luciana Méndez, Ernesto G Mata
No abstract text is available yet for this article.
November 8, 2010: Journal of Combinatorial Chemistry
P Jake Slavish, Jeanine E Price, Parimala Hanumesh, Thomas R Webb
No abstract text is available yet for this article.
November 8, 2010: Journal of Combinatorial Chemistry
Xu Zhu, Xiao-Ping Xu, Chang Sun, Hai-Ying Wang, Kai Zhao, Shun-Jun Ji
A novel and efficient method has been developed for the direct construction of imino-pyrrolidine-thione scaffold via the coupling of isocyanides, heterocyclic thiols, and gem-dicyano olefins. Smiles rearrangement followed by intramolecular cyclization leads directly to formation of the core structure. A water-acceleration effect is observed, promoting most of the reactions to go to completion within a short reaction time.
November 8, 2010: Journal of Combinatorial Chemistry
Ya-Shan Hsiao, Gorakh S Yellol, Li-Hsun Chen, Chung-Ming Sun
A new multidisciplinary synthetic approach comprising polymer-support synthesis, microwave-assisted synthesis, and multicomponent condensation facilitates synthesis of triaza-fluorenes library with a set of advantages such as rapid process, simple purification, and structural diversity in one shot. Microwave-assisted multistep synthetic protocol was used to construct the benzimidazole ring on soluble polymer support using activated aryl-fluorides. The PEG anchored aryl fluoride was condensed with selective primary amines via an ipso-fluoro displacement reaction followed by reduction of nitro group...
September 13, 2010: Journal of Combinatorial Chemistry
Yaguang Bai, Jing Zeng, Jimei Ma, Bala Kishan Gorityala, Xue-Wei Liu
A direct and efficient approach to 1-aminoindolizines through three-component one-pot reaction of heteroaryl aldehydes, secondary amines, and terminal alkynes catalyzed by AgBF(4) has been developed. Desired products were obtained in moderate to excellent yields. Similar aminoindolizines products were afforded from trimethylsilyl protected alkyne substrates as well. This methodology provides a rapid access to construct a diversity-oriented library of indolizines.
September 13, 2010: Journal of Combinatorial Chemistry
Kodumuru Vishnumurthy, Alexandros Makriyannis
Microwave-promoted novel and efficient one-step parallel synthesis of dibenzopyranones and heterocyclic analogues from bromo arylcarboxylates and o-hydroxyarylboronic acids via Suzuki-Miyaura cross coupling reaction is described. Spontaneous lactonization gave dibenzopyranones and heterocyclic analogues bearing electron-donating and -withdrawing groups on both aromatic rings in good to excellent yields.
September 13, 2010: Journal of Combinatorial Chemistry
Florence S Gaucher-Wieczorek, Ludovic T Maillard, Bernard Badet, Philippe Durand
The parallel synthesis of O-aryloxyamines remains an unfulfilled need in the field of medicinal chemistry and fragment-based approaches. To fill this gap a solution-phase two-step process based on (1) a copper-catalyzed cross-coupling of aryl boronic acids with a fluorous tagged N-hydroxyphthalimide, and (2) a supported aminolysis was designed and optimized using Taguchi's method. A library of O-aryloxyamines was synthesized in high yields with high purity and diversity.
September 13, 2010: Journal of Combinatorial Chemistry
Minoo Dabiri, Peyman Salehi, Mahboobeh Bahramnejad, Fatemeh Sherafat
A facile and highly efficient method for one-pot four-component synthesis of triazolyl methoxy phenylquinazolines is described. A mixture of aromatic propargylated aldehydes, different azides, 2-aminobenzophenone derivatives, and ammonium acetate were condensed in the presence of catalytic amounts of acidic ionic liquid, 1-methylimidazolium trifluoroacetate, ([Hmim]TFA), and Cu(OAc)(2)/sodium ascorbate to afford the corresponding products in excellent yields. This methodology is highly efficient for structurally diverse azides...
September 13, 2010: Journal of Combinatorial Chemistry
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