- HETEROCYCLIC AMIDE COMPOUND
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PROBLEM TO BE SOLVED: To provide a heterocyclic amide compound useful as an active ingredient of a herbicide. SOLUTION: The present disclosure provides a heterocyclic amide compound represented by the following formula or a salt thereof. Q-N(R3)-C(=X)-W (Q: a substituted/unsubstituted 1,3,4-oxadiazole, 1,2,5-oxadiazole or the like. W: a substituted/unsubstituted [1,2,4]triazolo[4,3-a]pyridine or the like. X: O, S. R3: H, C1-C6 alkyl or the like). SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
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Paragraph 0223
(2021/10/02)
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- HETEROCYCLIC AMIDE COMPOUND
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PROBLEM TO BE SOLVED: To provide a herbicide that reliably has an effect on various weeds at a reduced dosage, has reduced trouble such as soil pollution and influence on succeeding crops, and is highly safe. SOLUTION: The present invention provides a heterocyclic amide compound represented by the following formula and a herbicide containing the same. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
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Paragraph 0243
(2020/10/31)
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- Development of 11C-Labeled ω-sulfhydryl fatty acid tracer for myocardial imaging with PET
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[11C]-S-methyl-16-thiopalmitic acid (a) was developed with excellent heart-to-background uptake ratios and higher retention in heart. Myocardial uptake and metabolism of the tracer is markedly higher CPT I dependent. When compared to [11C]-S-methyl-14-thiomyristic acid (b), [11C]-S-methyl-12-thiododecanoic acid (c) and [11C]-palmitate, a showed an early high uptake and a significantly slower late clearance in heart and a prolonged myocardial elimination half-life (30 min). Analysis of heart tissue and urine samples showed that a was metabolized via beta-oxidation in myocardium. Small animal PET images of the accumulation of a in the rat myocardium were clearly superior to [11C]-palmitate. These initial studies suggest that a could be a potentially useful clinical PET tracer to assess myocardial fatty acid metabolism.
- Wu, Xiangxiang,Wang, Peizhi,Liu, Ruixin,Zeng, Huahui,Chao, Fangfang,Liu, Hao,Xu, Caiyun,Hou, Haifeng,Yao, Qiong
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p. 1657 - 1666
(2017/11/17)
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- A cogeneration process for producing sulfur and sulfur on behalf of acetate acid diester method (by machine translation)
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The invention technical field of chemical synthesis, in particular relates to a methionine as raw material production process for producing sulfur and sulfur on behalf of acetate acid diester method. The invention states the payment proportional to production for preparing sulfur and sulfur on behalf of acetate acid diester method, in order to methionine and halogenated acetic acid as the raw material, the preparation comprising a homoserine lactone hydrohalide salt (IV), a sulfur acetate (I) and sulfur on behalf of the b b acid diester (II) of the three kinds of chemical products, and each between the products easy to separate and purify. (by machine translation)
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Paragraph 0076; 0078
(2018/12/02)
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- HETEROCYCLIC AMIDO COMPOUND
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PROBLEM TO BE SOLVED: To provide a novel pesticide, especially a herbicide. SOLUTION: There are provided a heterocycle amide compound such as 3-isopropyl-N-(5-methyl-1, 3, 4-oxadiazole-2-yl)-5-(trifluoromethyl)-[1, 2, 4]triazolo [4,3-a] pyridine-8-carboxamide (compound No.1-004), 3-isopropyl-N-(5-methyl-1, 3, 4-oxadiazole-2-yl)-5-(methylthio)-[1,2,4] triazolo [4,3-a] pyridine-8-carboxamide (compound No.1-009), and a herbicide containing them. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0211
(2018/06/28)
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- A designed amide as an aldol donor in the direct catalytic asymmetric aldol reaction
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The direct catalytic asymmetric aldol reaction offers efficient access to β-hydroxy carbonyl entities. Described is a robust direct catalytic asymmetric aldol reaction of α-sulfanyl 7-azaindolinylamide, thus affording both aromatic and aliphatic β-hydroxy amides with high ee values. The design of this transformation features a cooperative interplay of a soft and a hard Lewis acid, which together facilitate the challenging chemoselective enolization by a hard Bronsted base.
- Weidner, Karin,Kumagai, Naoya,Shibasaki, Masakatsu
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supporting information
p. 6150 - 6154
(2014/06/23)
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- Synthesis and biological activities of 3-substituted analogues of tenuazonic acid
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A series of tenuazonic acid analogues in which the acetyl group was replaced with electron-withdrawing substituents have been synthesized with the aim of obtaining molecules with various bioactivities. Substituents such as cyano, sulfonyl, and amido were introduced at the 3-position of the pyrrolidine-2,4-dione nucleus of tenuazonic acid. 3-Cyano and sulfonyl pyrrolidine-2,4-dione compounds (2 and 6) were prepared via a Dieckmann cyclization as key step. 3-Amido pyrrolidine-2,4-dione compounds (9) were prepared by a microwave-assisted amidation reaction from corresponding 3-carboxylate derivative. The target compounds were evaluated; their herbicidal, fungicidal, and insecticidal activities, and the preliminary bioassay data showed that some 3-cyanopyrrolidine-2,4-diones 2 gave good insecticidal activity, whereas some 3-amido compounds 9 exhibited moderate to strong fungicidal activity against Pythium dissimile at 20 mg/L.
- Liu, Yu-Xiu,Cui, Zhi-Peng,Zhao, Hua-Ping,Li, Yong-Hong,Gu, Yu-Cheng,Wang, Qing-Min
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p. E209-E215
(2014/11/07)
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- 3-Thiolated 2-azetidinones: Synthesis and in vitro antibacterial and antifungal activities
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A series of 3-thiolated β-lactams were synthesized by [2+2] ketene-imine cycloaddition reaction from S-substituted mercaptoacetic acids and Schiff bases. Then, some of the 3-methylthio β-lactams were converted to 3-(methylsulfinyl) β-lactams and 3-(methylsulfonyl) β-lactams using m-CPBA under different reaction conditions. All the compounds were characterized by spectral data and elemental analyses and were evaluated for their in vitro antibacterial and antifungal activities against pathogenic strains including Staphylococcus aureus (Methicillin resistant strain). The preliminary screening results indicated that some of these compounds demonstrated moderate to very good antibacterial and antifungal activities.
- Zarei, Maaroof,Mohamadzadeh, Masoud
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experimental part
p. 5832 - 5840
(2011/08/10)
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- Fully enzymatic resolution of chiral amines: Acylation and deacylation in the presence of Candida antarctica lipase B
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A fully enzymatic methodology for the resolution of chiral amines has been demonstrated. Candida antarctica lipase B (CaLB)-catalyzed acylation with N-methyl-and N-phenylglycine, as well as analogues having the general formula R1-X-CH2CO2R2 (R1 = Me, Ph; X = O, S) afforded the corresponding enantioenriched amides, which were subsequently enzymatically hydrolyzed. Surprisingly, CaLB also proved to be the catalyst of choice for this latter step. The heteroatom in the acyl donor profoundly influences both the enzymatic acylation and deacylation; the O-substituted reagents performed best with regard to enantioselectivity as well as reaction rate in synthesis and hydrolysis.
- Ismail, Hilda,Lau, Rute Madeira,Van Rantwijk, Fred,Sheldon, Roger A.
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experimental part
p. 1511 - 1516
(2009/08/07)
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- The first asymmetric total syntheses and determination of absolute configurations of xestodecalactones B and C
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The first efficient asymmetric total syntheses of xestodecalactones B and C have been accomplished in 10 steps with an overall yield of 22 and 20.2%, respectively. The key steps involve the utility of Evans oxazolidinone-mediated syn-aldol condensations to establish the C-9 configuration and the macrolide ring formation by intramolecular acylation. The absolute configurations of xestodecalactones B and C have been determined via these syntheses.
- Liang, Qiren,Zhang, Jiyong,Quan, Weiguo,Sun, Yongquan,She, Xuegong,Pan, Xinfu
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p. 2694 - 2697
(2007/10/03)
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- Exploring the synthetic applicability of a cyanobacterium nitrilase as catalyst for nitrile hydrolysis
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The substrate specificity and synthetic applicability of the nitrilase from cyanobacterium Synechocystis sp. strain PCC 6803 have been examined. This nitrilase catalyzed the hydrolysis of both aromatic and aliphatic nitriles to the corresponding acids in high yields. Furthermore, the stereoselective hydrolysis of phenyl-substituted β-hydroxy nitriles to (S)-enriched β-hydroxy carboxylic acids and selective hydrolysis of α,ω- dinitriles with five or less methylene groups to ω-cyano carboxylic acids have been achieved. This suggested that nitrilase from Synechocystis sp. PCC 6803 could be a useful enzyme catalyst for the "green" nitrile hydrolysis. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
- Mukherjee, Chandrani,Zhu, Dunming,Biehl, Edward R.,Hua, Ling
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p. 5238 - 5242
(2007/10/03)
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- Enzymatic nitrile hydrolysis catalyzed by nitrilase ZmNIT2 from maize. An unprecedented β-hydroxy functionality enhanced amide formation
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To explore the synthetic potential of nitrilase ZmNIT2 from maize, the substrate specificity of this nitrilase was studied with a diverse collection of nitriles. The nitrilase ZmNIT2 showed high activity for all the tested nitriles except benzonitrile, producing both acids and amides. For the hydrolysis of aliphatic, aromatic nitriles, phenylacetonitrile derivatives and dinitriles, carboxylic acids were the major products. Unexpectedly, amides were found to be the major products in nitrilase ZmNIT2-catalyzed hydrolysis of β-hydroxy nitriles. The hydrogen bonding between the hydroxyl group and nitrogen in the enzyme-substrate complex intermediates that disfavors the loss of ammonia and formation of acyl-enzyme intermediate, which was further hydrolyzed to acid, was proposed to be responsible for the unprecedented β-hydroxy functionality assisted high yield of amide formation.
- Mukherjee, Chandrani,Zhu, Dunming,Biehl, Edward R.,Parmar, Rajiv R.,Hua, Ling
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p. 6150 - 6154
(2007/10/03)
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- 4-METHOXY-5-METHYL-PYRAN-3-OL NATURAL PRODUCTS AND DERIVATIVES THEREOF
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Novel antibiotic substances, including novel natural products, having the general formula wherein R1 and R2 are as defined herein, are disclosed. These compounds have been found to be cytochrome P450 inhibitors.
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- Degenerate Transesterification of 3,5-Dimethylphenolate/3,5-Dimethylphenyl Esters in Weakly Polar, Aprotic Solvents. Reactions of Aggregates and Complex-Induced Proximity Effects
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The rates of exchange of the 3,5-dimethylphenolate ion between lithium 3,5-dimethylphenolate-d6 and a series of 3,5-dimethylphenyl esters have been determined in the weakly polar, aprotic solvents dioxolane, dimethoxyethane (DME), tetrahydrofuran (THF), and pyridine. The esters include the propionate, butyrate, methoxyacctate, β-methoxypropionate, 4-methoxybutyrate, 2-tetrahydrofuroate, 2-furoate, (N,N-dimethylamino)acetate, (methylthio)acetate, 2- and 4-pyridine-carboxylates, 2-pyridylacetate, 4-pyridylacetate, phenylacetate, andp-methoxy-,p-chloro-, and p-(trifluoromethyl)phenylacetates. The rates and kinetic orders of the reactions of 3,5-dimethylphenyl propionate in various solvents at 35°C gave the following second-order rate constants (104k2, L mol-1 sec-1) for the following major aggregate species: THF tetramer, 6.5; DME tetramer, 3.3 (40°C); dioxolane, 13, hexamer, 71; pyridine tetramer, 2.2, dimer, 29. For 3,5-dimethylphenyl β-methoxypropionate, the order of reactivity is dioxolane > DME > THF. These results are interpreted in terms of a preequilibrium in which a solvent on lithium in the tetramer is replaced by the ester. The rates of transesterification have been compared with the rates of hydrolysis in 30% aqueous ethanol for the above series of esters. Those esters that have a second Lewis base center proximal to the ester function show significantly increased reactivity in transesterification, which is attributed to a complex-induced proximity effect.
- Jackman,Petrei,Smith
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p. 3451 - 3458
(2007/10/02)
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- POLAROGRAPHY OF METHYLENE BIS(THIOACETIC ACID) IN AQUEOUS SOLUTIONS AND IN AQUEOUS ORGANIC SOLVENT MIXTURES
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The polarographic behaviour of methylene bis (thioacetic acid) (referred to herein as R-S-CH2-S-R) at the d.m.e. has been studied in aqueous and in 20 per cent v/v methanol, ethanol, acetonitrile, DMF and DMSO media in the presence of 0.1 M KNO3 and 0.001 per cent Triton-X-100.The effects of changes in pH, concentration, mercury pressure and different supporting electrolytes, viz.KNO3, KCl, NaCl, NaClO4 (CH3)4NBr and (C2H5)4NBr on the wave characteristics and the mechanism of the electrode reaction, have been studied.Well defined reversible and diffusion controlled cathodic waves were obtained between pH 11 and 12.80.Evidences obtained show that the cathodic wave of R-S-CH2-S-R at the d.m.e. in aqueous solutions and aqueous organic solvent mixtures is due to the reduction of R-S-CH2-S-R to RSH.The diffusion current is linearly related to the concentration of R-S-CH2-S-R in the 0.33-2 mM concentration range and may thus be used for quantitative determination.
- Saxena, R. S.,Parikh, R. D.,Gupta, K. C.
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p. 213 - 222
(2007/10/02)
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- Mass Spectrometry of 2-Alkylthio-2-methylpropanoic Acids and Their Esters and Amides. Structural and Steric Effects on the McLafferty Rearrangement
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The electron ionization mass spectra (MS) of S-methylated derivatives of N-(2-mercapto-2-methylpropanoyl)-L-cysteine and 2-alkylthio-2-methylpropanoic acids, as well as their esters and amides, were examined.Use of the deuterium labeling technique and accurate mass measurement supported the proposed fragmentation pathways.Extensive loss of CH2S from a molecular ion by the McLafferty rearrangementof a primary hydrogen is important in the MS of S-methyl compounds of amide derivatives.It was demonstrated that the intensity of the rearrangement ion decreases in the order of amide, ester, and acid, and in the case if amides the reaarangement is suppressed by the nonbonded interaction between methyl groups on the α carbon and the amide nitrogen.Keywords-N-(2-mercapto-2-methylpropanoyl)-L-cysteine; 2-alkylthio-2-methylpropanoic acid and methyl ester; 2-alkylthio-2-methylpropanamide; electron impact mass spectrometry; McLafferty rearrangement; steric interaction
- Mori, Yuji,Fujiwara, Shigeru,Miyachi, Toshiko,Kitanishi, Hiroyuki,Oya, Masayuki,et al.
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p. 1505 - 1517
(2007/10/02)
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