cas 1193-92-6, 3-PYRIDINEALDOXIME | Articles data

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Isoxazoles: Synthesis, evaluation and bioinformatic design as acetylcholinesterase inhibitors
Objectives Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of Alzheimer's disease. In this study, nine isoxazoles derivatives were tested for their in-vitro AChE activity. The molecular docking showed the interaction of the compounds with the active site. Methods The isoxazoles were synthesized using 1,3-dipolar cycloaddition in the presence of sodium hypochlorite. They were also isolated and characterized by spectroscopic methods. The in-vitro activity was measured by an adapted version of Ellman's assay. Key findings The isoxazoles are described as inhibitors of AChE. The most potent compound in the series exhibited a moderate inhibitory activity (50% inhibitory concentration = 134.87 μm). The design of new compounds was created by using the RACHEL module of the SYBYL software. Conclusions Our research provided enough evidence of the efficacy of isoxazoles as AChE inhibitors. The isoxazoles were synthesized and evaluated as inhibitors of AChE. The docking study based on a novel series of complexes isoxazole with AChE from Electroporus electricus has demonstrated that the ligand bind is similar to the compounds used as reference. To find new candidates with the isoxazole core that act as inhibitors of AChE, part of the structure of the compound 9 was used for de-novo design. Molecular docking models of the ligand-AChE complexes suggest that the compound 10 is located on the periphery of the AChE active site.
Gutiérrez, Margarita,Matus, María Francisca,Poblete, Tomas,Amigo, Jessica,Vallejos, Gabriel,Astudillo, Luis
p. 1796 - 1804
(2013)
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AN IMPROVED PROCESS FOR PREPARATION OF PURE ALDOXIME
The present invention relates to an improved process for preparing aldoximes of formula (I) with high purity and high yield. The improved process for preparing aldoxime is fast, simple, highly efficient, and reproducible. The improved process for the preparation of aldoxime, which is synthesized in the higher yield under oximation reaction of aldehyde with hydroxylamine hydrochloride merely in aqueous medium using of in situ heat generation.
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Page/Page column 14-15

(2021/06/22)

Electrochemical synthesis of 1,2,4-oxadiazoles from amidoximes through dehydrogenative cyclization
A convenient and efficient method for the generation of the iminoxy radical through anodic oxidation was developed for the synthesis of 3,5-disubstituted 1,2,4-oxadiazoles fromN-benzyl amidoximes. The transformation proceeds through 1.5-Hydrogen Atom Transfer (1,5-HAT) and intramolecular cyclization. The process features simple operation, mild conditions, broad substrate scope and high functional group compatibility, and provides a facile and practical way for the preparation of 1,2,4-oxadiazoles.
Hu, Aixi,Jiang, chan,Li, mingfang,Xu, Leitao,Ye, Jiao,Yi, Yangjie
supporting information
p. 10611 - 10616
(2021/12/27)

PROCESS FOR REGENERATING A LIQUID ABSORBENT
The invention provides a process for regenerating a liquid absorbent, comprising: contacting the liquid absorbent with a hydrophobic medium, wherein the liquid absorbent comprises at least one amine of Formula (I) and degradation product thereof comprising at least one imine of Formula (II), wherein each Ar is independently an aromatic group and each R is independently selected from hydrogen, an organyl group and NH2; and selectively extracting the degradation product into or through the hydrophobic medium.
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(2020/11/12)

1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors
Two series of saccharin/isoxazole and saccharin/isoxazoline hybrids were synthesized by 1,3-dipolar cycloaddition. The new compounds showed to be endowed with potent and selective inhibitory activity against the cancer-related human carbonic anhydrase (hCA) IX and XII isoforms in the nanomolar range, while no affinity was encountered for off-targets, such as hCA I and II. Successive enantioseparation on a milligram scale of the most representative compounds led to the discovery that (S)-isomers were more potent than their corresponding (R)-enantiomers. Lastly, molecular modeling studies were conducted to define those structural requirements that were responsible for the discrimination among selected human isoforms of carbonic anhydrases. Two nanomolar hCA IX and XII inhibitors were also screened for their selective toxicity against non tumoral primary cells (fibroblasts) and against a breast adenocarcinoma cell line (MCF7) in hypoxic environment. The efficacious combination of these compounds with doxorubicin on MCF7 cells was demonstrated after 72 h of treatment.
D'Ascenzio, Melissa,Secci, Daniela,Carradori, Simone,Zara, Susi,Guglielmi, Paolo,Cirilli, Roberto,Pierini, Marco,Poli, Giulio,Tuccinardi, Tiziano,Angeli, Andrea,Supuran, Claudiu T.
p. 2470 - 2488
(2020/03/31)

Chlorotropylium Promoted Conversions of Oximes to Amides and Nitriles
Chlorotropylium chloride as a catalyst for the transformations of oximes, ketones, and aldehydes to their corresponding amides and nitriles in excellent yields (up to 99 %) and in short reaction times (mostly 10–15 min). Oximes were electrophilically attacked on the hydroxyl oxygen by chlorotropylium. The produced tropylium oxime ethers were the key intermediates, of which the ketoxime ether led to amide through Beckmann rearrangement, and the aldoxime ether led to nitrile by nitrogen base DBU assisted formal dehydration. This chlorotropylium activation protocol offered general, mild, and efficient avenues bifurcately from oximes to both amides and nitriles by one organocatalyst.
Xu, Jiaxi,Gao, Yu,Li, Zhenjiang,Liu, Jingjing,Guo, Tianfo,Zhang, Lei,Wang, Haixin,Zhang, Zhihao,Guo, Kai
p. 311 - 315
(2020/01/25)

Synthetic method for nicotinamide
The invention belongs to the field of organic chemistry, and discloses a synthetic method for nicotinamide. The method comprises the following steps: using ethanol as a solvent, using 3-methylpyridineas a raw material, introducing a dried nitrosyl chloride gas, performing a photonitrosation-isomerization reaction under irradiation of visible light at temperature of 0-30 DEG C, after the reactionis completed, introducing a nitrogen gas, adding an alkali to adjust pH of the reaction solution to be 6-9, and performing filtration to obtain a filtrate; and adding a copper salt and a nitrile intothe filtrate as a catalyst, performing heating, performing reflux, performing an aldoxime Beckmann rearrangement reaction, after the reaction is completed, adding ethyl acetate crystals into the reaction solution, performing filtration to obtain a crude product of the nicotinamide, and performing recrystallization on the crude product of the nicotinamide to obtain a pure product of the nicotinamide. The synthetic method provided by the invention has mild reaction conditions, a simple process and a high yield, can obtain the high-purity nicotinamide product, has less three waste (waste water, waster gas and solid waste) and high economy, and is suitable for industrialized large-scale production.
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Sheet 0028; 0029; 0031; 0032; 0034; 0035

(2018/09/11)

Synthesis and biological evaluation of (3-arylisoxazol-5-yl)methyl 6-fluoro-4-oxo-4H-chromene-2-carboxylates as antioxidant and antimicrobial agents
A series of novel (3-arylisoxazol-5-yl)methyl 6-fluoro-4-oxo-4H- -chromene-2-carboxylate derivatives (C1-C12) were synthesized by the Cu(I)- -catalyzed reaction of in situ generated nitrile oxides with prop-2-ynyl 6-fluoro- 4-oxo-4H-chromene-2-carboxylate in good yields and their antioxidant and antimicrobial activities were investigated. Among all the synthesized compounds, C1 (IC50: 16.43±0.57 μM) and C12 (IC50:15.98±0.72 μM) registered good antioxidant activity as compared to the standard drug trolox. Compounds C1, C3 and C6 registered very good inhibition against all the tested Gram-positive and Gram-negative bacterial strains with MIC values ranging from 9.375 to 37.5 μg mL-1. Compounds C7-C11 registered good inhibition against Bacillus subtilis and Staphylococcus aureus with MIC values ranging from 18.75 to 37.5 μg mL-1. Compounds C10 and C11 against Pseudomonas aeroginosa showed more prominent activity than the standard drug penicillin (MIC: 12.5 μg mL-1) with an MIC value of 9.375 μg mL-1 (≈ 1.33-fold more potent than penicillin). Compounds C7-C9 registered good to moderate antifungal activity against the four tested fungal strains with MIC values ranging from 18.75 to 37.5 μg mL-1.
Battula, Kumaraswamy,Narsimha, Sirassu,Nagavelli, Vasudeva Reddy,Rao, Mutheneni Srinivasa
p. 1 - 12
(2017/02/15)

Catalytic Enantioselective [3 + 2] Cycloaddition of α-Keto Ester Enolates and Nitrile Oxides
An enantioselective [3 + 2] cycloaddition reaction between nitrile oxides and transiently generated enolates of α-keto esters has been developed. The catalyst system was found to be compatible with in situ nitrile oxide-generation conditions. A versatile array of nitrile oxides and α-keto esters could participate in the cycloaddition, providing novel 5-hydroxy-2-isoxazolines in high chemical yield with high levels of diastereo- and enantioselectivity. Notably, the optimal reaction conditions circumvented concurrent reactions via O-imidoylation and hetero-[3 + 2] pathways.
Bartlett, Samuel L.,Sohtome, Yoshihiro,Hashizume, Daisuke,White, Peter S.,Sawamura, Miki,Johnson, Jeffrey S.,Sodeoka, Mikiko
supporting information
p. 8661 - 8666
(2017/07/06)

Asymmetric Nitrone Synthesis via Ligand-Enabled Copper-Catalyzed Cope-Type Hydroamination of Cyclopropene with Oxime
We report realization of the first enantioselective Cope-type hydroamination of oximes for asymmetric nitrone synthesis. The ligand promoted asymmetric cyclopropene "hydronitronylation" process employs a Cu-based catalytic system and readily available starting materials, operates under mild conditions and displays broad scope and exceptionally high enantio- and diastereocontrol. Preliminary mechanistic studies corroborate a CuI-catalytic profile featuring an olefin metalla-retro-Cope aminocupration process as the key C-N bond forming event. This conceptually novel reactivity enables the first example of highly enantioselective catalytic nitrone formation process and will likely spur further developments that may significantly expedite chiral nitrone synthesis.
Li, Zhanyu,Zhao, Jinbo,Sun, Baozhen,Zhou, Tingting,Liu, Mingzhu,Liu, Shuang,Zhang, Mengru,Zhang, Qian
supporting information
p. 11702 - 11705
(2017/09/07)

Synthesis and antiproliferative properties of isoxazole analogs containing dibenzosuberane moiety
A series of twelve novel isoxazole analogs containing dibenzosuberane moiety were synthesized using convergent synthesis approach. Newly synthesized compounds were well characterized by mass spectroscopy, IR and NMR spectroscopy. All the compounds were screened for their antiproliferative property against HepG2 and HeLa cell lines. Among them, compounds 7a, 7b, 7c, 7g and 7h were found active against both HepG2 and HeLa cell lines. Graphical Abstract: Twelve analogs of isoxazole containing dibenzosuberane moiety (7a-l) were synthesized, characterized and evaluated for their antiproliferative activity. [Figure not available: see fulltext.]
Moger, Manjunath,Pradhan, Ashok,Singh, Apoorva,Govindaraju, Darshan Raj Chenna,Hindupur, Rama Mohan,Pati, Hari N.
p. 449 - 455
(2016/02/19)

Synthesis of 1,4,2-Oxathiazoles via Oxidative Cyclization of Thiohydroximic Acids
An oxidative formation of 1,4,2-oxathiazoles from readily available thiohydroximic acids is reported. A variety of alkyl, aryl, and heteroaryl substituents are well tolerated for both the thiohydroximic acid and activating fragments, and the reaction has been demonstrated on gram-scale. This reaction represents the only method currently available to prepare a diverse set of oxathiazoles and expands the chemistry of C-H oxidation via appended N-OH functional groups. Finally, we also demonstrate the rapid preparation of a 1,4,2-oxathiazole analog of an anticancer lead molecule.
Lemercier, Bérénice C.,Pierce, Joshua G.
supporting information
p. 4542 - 4545
(2015/09/28)

Efficient synthesis of bis-isoxazole ethers via 1,3-dipolar cycloaddition catalysed by Zn/Zn2+ and their antifungal activities
An efficient method was developed for synthesising isoxazoles. A series of novel bis-isoxazole ether compounds VI, VII and VIII were synthesised starting from different substituted aldehydes (I) via a 1,3-dispolar cycloaddition using Zn/Zn2+ as a catalyst; these were characterised by FT-IR, HRMS, 1H NMR and 13C NMR spectroscopy. In addition, the antimicrobial properties of the synthesised products were investigated. The synthesised compounds exhibited significant antifungal activities in comparison with the standard drugs, fluconazole and itraconazole. It was found that Candida albicans was sensitive to 2-substituted phenyl bis-isoxazole ethers bearing pyridyl.
Zhang, Da-Wei,Lin, Feng,Li, Bo-Chao,Liu, Hong-Wei,Zhao, Tian-Qi,Zhang, Yu-Min,Gu, Qiang
p. 1500 - 1511
(2015/09/15)

Synthesis of Nitriles from Aldoximes and Primary Amides Using XtalFluor-E
The dehydration reaction of aldoximes and amides for the synthesis of nitriles using [Et2NSF2]BF4 (XtalFluor-E) is described. Overall, the reaction proceeds rapidly (normally 1 h) at room temperature in an environmentally benign solvent (EtOAc) with only a slight excess of the dehydrating agent (1.1 equiv). A broad scope of nitriles can be prepared, including chiral nonracemic ones. In addition, in a number of cases, further purification of the nitrile after the workup was not required.
Keita, Massaba,Vandamme, Mathilde,Paquin, Jean-Fran?ois
p. 3758 - 3766
(2015/11/28)

Mechanochemical and conformational study of N-heterocyclic carbonyl-oxime transformations
New mechanochemical pathways for the transformation of six N-heterocyclic carbonyl compounds into oximes using hydroxylamine hydrochloride were explored. Reactions were performed first without any base since the heterocyclic moieties (imidazole, benzimidazole, pyridine and quinuclidine) have an intrinsic basic nitrogen atom. This green, solvent free method was suitable for all compounds (up to quantitative yields) except for N-benzyl substituted imidazole and benzimidazole-2-carbaldehyde. For the slower reacting aldehydes, reactions with liquid assisted grinding and addition of sodium hydroxide were performed as well. Conformational analysis and quantum-chemical calculations revealed steric and electronic reasons for the lower reactivity of N-benzyl substituted derivatives.
Primoi, Ines,Hrenar, Tomica,Baumann, Kreimir,Krito, Lucija,Krii, Ivana,Tomi, Srdlanka
p. 153 - 160
(2015/02/19)

Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists
A novel set of compounds containing a 4,5-dihydro-5-methylisoxazoline have been successfully designed as VLA-4 receptor antagonists. Compound (14p) had a high receptor binding affinity of 4 nM and also found to be metabolically stable in vitro.
Soni, Ajay,Rehman, Abdul,Naik, Keshav,Dastidar, Sunanda,Alam,Ray, Abhijit,Chaira, Tridib,Shah, Vanya,Palle, Venkata P.,Cliffe, Ian A.,Sattigeri, Viswajanani J.
p. 1482 - 1485
(2013/03/14)

A versatile and green mechanochemical route for aldehyde-oxime conversions
A robust, facile and solvent-free mechanochemical path for aldehyde-oxime transformations using hydroxylamine and NaOH is explored; the method is suitable for aromatic and aliphatic aldehydes decorated with a range of substituents. This journal is
Aakeroey, Christer B.,Sinha, Abhijeet S.,Epa, Kanishka N.,Spartz, Christine L.,Desper, John
supporting information
p. 11289 - 11291,3
(2012/12/12)

Ruthenium-catalyzed rearrangement of aldoximes to primary amides in water
The rearrangement of aldoximes to primary amides has been studied using the readily available arene-ruthenium(II) complex [RuCl2(η 6-C6Me6){P(NMe2)3}] (5 mol %) as catalyst. Reactions proceeded cleanly in pure water at 100 °C without the assistance of any cocatalyst, affording the desired amides in high yields (70-90%) after short reaction times (1-7 h). The process was operative with both aromatic, heteroaromatic, α,β-unsaturated, and aliphatic aldoximes and tolerated several functional groups. Reaction profiles and experiments using 18O-labeled water indicate that two different mechanisms are implicated in these transformations. In both of them, nitrile intermediates are initially formed by dehydration of the aldoximes. These intermediates are then hydrated to the corresponding amides by the action of a second molecule of aldoxime or water. A kinetic analysis of the rearrangement of benzaldoxime to benzamide is also discussed.
Garcia-Alvarez, Rocio,Diaz-Alvarez, Alba E.,Borge, Javier,Crochet, Pascale,Cadierno, Victorio
p. 6482 - 6490
(2012/10/30)

Synergistic catalysis by polyoxometalate-intercalated layered double hydroxides: Oximation of aromatic aldehydes with large enhancement of selectivity
Sandwich-type polyoxometalates intercalated in layered double hydroxides have been shown to exhibit synergistic catalysis of the oximation of aromatic aldehydes with a large enhancement of selectivity.
Zhao, Shen,Xu, Junhua,Wei, Min,Song, Yu-Fei
experimental part
p. 384 - 389
(2011/04/16)

Stereospecific synthesis of syn -α-oximinoamides by a three-component reaction of isocyanides, syn -chlorooximes, and carboxylic acids
A stereospecific multicomponent reaction among isocyanides, syn-chlorooximes, and carboxylic acids provides an efficient synthesis of biologically relevant syn-α-oximinoamides.
Pirali, Tracey,Mossetti, Riccardo,Galli, Simona,Tron, Gian Cesare
supporting information; experimental part
p. 3734 - 3737
(2011/09/15)

Highly efficient cyclosarin degradation mediated by a β-cyclodextrin derivative containing an oxime-derived substituent
The potential of appropriately substituted cyclodextrins to act as scavengers for neurotoxic organophosphonates under physiological conditions was evaluated. To this end, a series of derivatives containing substituents with an aldoxime or a ketoxime moiety along the narrow opening of the β-cyclodextrin cavity was synthesized, and the ability of these compounds to reduce the inhibitory effect of the neurotoxic organophosphonate cyclosarin on its key target, acetylcholinesterase, was assessed in vitro. All compounds exhibited a larger effect than native β-cyclodextrin, and characteristic differences were noted. These differences in activity were correlated with the structural and electronic parameters of the substituents. In addition, the relatively strong effect of the cyclodextrin derivatives on cyclosarin degradation and, in particular, the observed enantioselectivity are good indications that noncovalent interactions between the cyclodextrin ring and the substrate, presumably involving the inclusion of the cyclohexyl moiety of cyclosarin into the cyclodextrin cavity, contribute to the mode of action. Among the nine compounds investigated, one exhibited remarkable activity, completely preventing acetylcholinesterase inhibition by the (-)-enantiomer of cyclosarin within seconds under the conditions of the assay. Thus, these investigations demonstrate that decoration of cyclodextrins with appropriate substituents represents a promising approach for the development of scavengers able to detoxify highly toxic nerve agents.
Zengerle, Michael,Brandhuber, Florian,Schneider, Christian,Worek, Franz,Reiter, Georg,Kubik, Stefan
supporting information; experimental part
p. 1543 - 1554
(2012/01/30)

Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists
This Letter describes the synthesis and evaluation of mGluR7 antagonists in the isoxazolopyridone series. In the course of modification in this class, novel solid support synthesis of the isoxazolopyridone scaffold was developed. Subsequent chemical modification led to the identification of several potent derivatives with improved physicochemical properties compared to a hit compound 1. Among these, 2 showed good oral bioavailability and brain penetrability, suggesting that 2 may be useful for in vivo study to elucidate the role of mGluR7.
Nakamura, Masayuki,Kurihara, Hideki,Suzuki, Gentaroh,Mitsuya, Morihiro,Ohkubo, Mitsuru,Ohta, Hisashi
scheme or table
p. 726 - 729
(2010/05/18)

Oxime Carbamate-Discovery of a series of novel FAAH inhibitors
A series of novel oxime carbamates have been identified as potent inhibitors of the key regulatory enzyme of the endocannabinoid signaling system, fatty acid amide hydrolase (FAAH). In this Letter, the rationale behind the discovery and the biological evaluations of this novel class of FAAH inhibitors are presented. Both in vitro and in vivo results of selected targets are discussed, along with inhibition kinetics and molecular modeling studies.1.
Sit,Conway, Charles M.,Xie, Kai,Bertekap, Robert,Bourin, Clotilde,Burris, Kevin D.
supporting information; experimental part
p. 1272 - 1277
(2010/06/17)

Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases
We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of Trypanosoma brucei brucei parasites in culture. A high resolution (1.75 A) co-crystal structure of 8a bound to cruzain reveals how the non-peptidic P2/P3 moiety in such analogs bind the S2 and S3 subsites of the protease, effectively recapitulating important binding interactions present in more traditional peptide-based protease inhibitors and natural substrates.
Bryant, Clifford,Kerr, Iain D.,Debnath, Moumita,Ang, Kenny K.H.,Ratnam, Joseline,Ferreira, Rafaela S.,Jaishankar, Priyadarshini,Zhao, DongMei,Arkin, Michelle R.,McKerrow, James H.,Brinen, Linda S.,Renslo, Adam R.
scheme or table
p. 6218 - 6221
(2010/06/19)

Biologically active hydroxymoyl chlorides as antifungal agents
Several oximes and oxime ethers have been developed as antimicrobial agents. A series of chlorooximes (hydroximoyl chlorides) have been synthesized and tested for antifungal activity under in-vitro conditions against Candida albicans, Candida parapsilosis, Candida glabrata, Candida krusei, Aspergillus fumigatus, Aspergilhis flaviis and Aspergillus niger. The derived antifungal activity has been compared with the corresponding oximes. The results show that most of the chlorooximes exhibit potent antifungal activity with anti-isomers showing better activity. It is observed that most of the chlorooximes show interesting antifungal activity (MICs ≤ 32 μg/mL) compared to oximes. Compound 3q (2,3-dimethoxy phenyl hydroxymoyl chloride) is the most active compound. This compound is active against all the Candida species (MIC 0.5 μg/mL) as well as filamentous fungi with MIC range of 2-4 μg/mL. This series of compounds are fungicidal in nature as evident from the MFC results.
Ismail, Tabasum,Shafi, Syed,Singh, Parvinder Pal,Qazi, Naveed Ahmed,Sawant, Sanghapal D.,Ali, Intzar,Khan, Inshad Ali,Kumar,Qazi, Ghulam Nabi,Alam, M. Sarwar
p. 740 - 747
(2008/12/20)

Synthetic inhibitors of cytochrome P-450 2A6: Inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization
A series of 3-heteroaromatic analogues of nicotine were synthesized to delineate structural and mechanistic requirements for selectively inhibiting human cytochrome P450 (CYP) 2A6. Thiophene, substituted thiophene, furan, substituted furan, acetylene, imidazole, substituted imidazole, thiazole, pyrazole, substituted pyrazole, and aliphatic and isoxazol moieties were used to replace the N-methylpyrrolidine ring of nicotine. A number of potent inhibitors were identified, and several exhibited high selectivity for CYP2A6 relative to CYP2E1, -3A4, -2B6, -2C9, -2C19, and -2D6. The majority of these inhibitors elicited type II difference spectra indicating the formation of a coordinate covalent bond to the heme iron. The majority of inhibitors were reversible inhibitors although several mechanism-based inactivators were identified. Most of the inhibitors were also relatively metabolically stable. X-ray crystal structures of CYP2A6 cocrystallized with three furan analogues bearing methanamino side chains indicated that the amine side chain coordinated to the heme iron. The pyridyl moiety was positioned to accept a hydrogen bond from Asn297, and all three inhibitors exhibited orthogonal aromatic-aromatic interactions with protein side chains. For comparison, the cocrystal structure of 4,4′-dipyridyl disulfide was also obtained and showed that the pyridine moiety could assume a different orientation than that observed for the 3-heteroaromatic pyridines examined. For the 3-heteroromatic pyridines, N-methyl and N,N-dimethyl amino groups increased the apparent Ki and distorted helix I of the protein. Substitution of a phenyl ring for the pyridyl ring also increased the apparent Ki, which is likely to reflect the loss of the hydrogen bonding interaction with Asn297. In contrast, inhibitory potency for other P450s was increased, and the selectivity of the phenyl analogues for CYP2A6 was decreased relative to the pyridyl compounds. The results suggest that inhibitors that compliment the active site features of CYP2A6 can exhibit significant selectivity for CYP2A6 relative to other human liver drug-metabolizing P450s.
Yano, Jason K.,Denton, Travis T.,Cerny, Matthew A.,Zhang, Xiaodong,Johnson, Eric F.,Cashman, John R.
p. 6987 - 7001
(2007/10/03)

Metalloporphyrin and heteropoly acid catalyzed oxidation of C=NOH bonds in an ionic liquid: Biomimetic models of nitric oxide synthase
Water soluble iron(III) porphyrins and phosphotungstic acid in an ionic liquid are effective catalysts for the H2O2 mediated oxidation of the CNOH bond in N-hydroxyarginine and other oximes. The carbonyl compounds generated as the oxidation products can be easily isolated from the reaction media. These systems serve as biomimetic models of nitric oxide synthase (NOS) and the catalyst immobilized in an ionic liquid can be easily recycled and reused.
Jain, Nidhi,Kumar, Anil,Chauhan, Shive M.S.
p. 2599 - 2602
(2007/10/03)

ZnO/CH3COCl: A new and highly efficient catalyst for dehydration of aldoximes into nitriles under solvent-free condition
A rapid and efficient synthesis of nitriles via dehydration from the corresponding aldoximes has been carried out in the presence of ZnO/CH 3COCl as catalyst under solvent free conditions in 83-95% yields. The zinc oxide (ZnO) powder can be re-used upto three times after simple washing with CH2Cl2.
Sarvari, Mona Hosseini
p. 787 - 790
(2007/10/03)

Rh-catalyzed one-pot and practical transformation of aldoximes to amides
Wilkinson's complex has been found to catalyze the one-pot transformation of aldoximes to the corresponding amides with high selectivity and efficiency under essentially neutral conditions.
Park, Soyoung,Choi, Yoon-aa,Han, Hoon,Yang, Soon Ha,Chang, Sukbok
p. 1936 - 1937
(2007/10/03)

bis(trichloromethyl)carbonate, an efficient activator for the one-pot conversion of aldehydes into nitriles under mild conditions
A single step conversion of aldehydes into the corresponding nitriles has been achieved in high yields using stoichiometric amounts of NH2OH·HCl, Et3N and bis(trichloromethyl)-carbonate at room temperature.
Bose, D. Subhas,Goud, P. Ravinder
p. 3621 - 3624
(2007/10/03)

6-chloro-2-(4,6-dimethoxypyrimidin-2-yl)oxybenzoic acid imino ester derivatives, processes for their production and a method for their application as herbicides
The present invention relates to 6-chloro-2-(4,6-dimethoxypyrimidin-2-yl)oxybenzoic acid iminoester derivative of the general formula I; process of their preparation and a method for their application as herbicides: STR1 wherein R and Q are as defined in the specification.
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(2008/06/13)

Novel 6-chloro-2-(4,6-dimethoxypyrimidin-2-yl) oxybenzoic acid ester derivatives, processes for their production an a method for their application as herbicides
The present invention relates to novel 6-chloro-2-(4,6-dimethoxypyrimidin-2-yl)oxybenzoic acid iminoester derivative of the general formula(I); processes for their preparation and a method for their application as herbicides: Therein, Q represents a straight or branched alkyl, alkenyl or cycloalkyl group having from 1 to 10 carbon atoms, preferably from 1 to 8 carbon atoms, which may be substituted with a (C1-C4)alkoxy or (C1-C4)alkylthio group; a (C1-C4)alkyl or (C2-C4)alkenylthio group; a phenylthio group; a phenyl(C1-C4)alkyl or phenyl(C2-C4)alkenylthio group; or a radical of the following formula: [wherein R1 and R2 are same or different each other and represent hydrogen or a halogen atom; or a group selected from the groups which comprised with a (C1-C4)alkyl, a (C2-C4)alkenyl, an acyl, an acyloxy, a (C1-C4)alkylthio, a nitro, a cyano, a phenyl and a phenoxy group, and which, if necessary, may be substituted with a halogen atom, a (C1-C4)alkyl, a (C1-C4)alkoxy or an acetal group; or R1 and R2 may constitute an acetal structure with carbon atoms to which R1 and R2 are linked.; and, n is 0 or 1.]; or a 5-6 membered ring system containing one or more hetero atoms such as oxygen, sulfur or nitrogen atom in the ring system, which may have one or more proper substituents such as a halogen atom, a (C1-C4)alkyl, a hydroxy, a nitro or a cyano group on its certain positions.; and, R represents a hydrogen or a halogen atom, a cyano group, or -Z -R3 [wherein, R3 represents a (C1-C4)alkyl, an alkoxy or alkenyloxyl group having from 1 to 8 carbon atoms, or a phenyl, a phenoxy or an amino group, or 5-6 membered hetero or aromatic ring system connecting to Z through out a (C1-C2)alkyl or alkoxy bridge, such as a phenyl, a furyl, a thienyl, pyrrolyl or pyranyl group, and which may have one or more proper substituents such as a halogen atom, a (C1-C4)alkyl, a hydroxy, a nitro or a cyano group on its certain positions, or R3 may be cyclized with Z and Q in some cases.; and, Z represents -O-, -S-, [wherein, R4 is a hydrogen atom, a (C1-C4)alkyl or a phenyl group, or constitutes a cyclic system containing an oxygen atom with R3]].
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(2008/06/13)