- In vitro inhibition studies of phytoene desaturase by bleaching ketomorpholine derivatives
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The herbicidal activities of homochiral steroisomeric 5-methyl-2-(3-trifluoromethylbenzyl)-3-ketomorpholine derivatives were investigated in vitro as inhibitors of phytoene desaturase, a key enzyme in carotenoid biosynthesis. It was demonstrated that ketomorpholines are classical bleaching compounds which directly inhibit phytoene desaturase, accumulating phytoene at the expense of colored carotenoids. Ketomorpholines interact with phytoene desaturase in a noncompetitive manner with respect to phytoene. A structure-activity investigation for in vitro inhibition of phytoene desaturase activity revealed that the relative and absolute stereochemistry is important for optimum inhibition for the 5-methyl derivatives, and that the distance of the phenyl group from the ketomorpholine ring is critical for the inhibitory potential. The average herbicidal score on 7 weeds and the in vitro I50 values related very well with the exception of two compounds. It was postulated that the discrepancies may possibly occur through modification in plants to compounds that are either more or less active herbicides.
- Sandmann, Gerhard,Mitchell, Glynn
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Read Online
- Method for preparing 3-ketomorpholine
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The invention relates to a method for preparing 3-ketomorpholine. The method comprises the following steps: protecting the amino group of ethanolamine firstly, then carrying out a reaction of amino group protected ethanolamine with alkyl haloacetate, performing deprotection on the prepared product, and performing ring closure so as to obtain 3-ketomorpholine. The method has the advantages of simple practical operation, low equipment requirements, high yield and low three waste, and is suitable for industrial large-scale production.
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Paragraph 0034; 0042; 0049-0050; 0052; 0059-0060; 0062-0080
(2019/03/26)
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- Method for preparing 3-morpholone
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The invention provides a method for preparing 3-morpholone. The method comprises the steps that halogen hydride removing is carried out on 2-halogenated ethylamine hydrohaloate under the condition oforganic solvent existing, an obtained reaction system and 2-glycollic acid ester are mixed and then subjected to amine ester exchange reaction to obtain 2-(2-hydroxyacetamido) halothane; ring closurereaction is carried out on the 2-(2-hydroxyacetamido) halothane under the condition of alkali reagent and organic solvent existing to obtain the 3-morpholone. The method for preparing the 3-morpholonehas the advantages that the technology side reaction is less, the product purification is convenient; the operation is simple, the safety is high, the method is environmentally friendly; raw materials are obtained easily, the price is low; the product yield is high (reaches 75.5%), the purity is high (reaches 99% or above), the method is suitable for the industrialized batch production, and the industrialized prospect is good.
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Paragraph 0046; 0048; 0054; 0056
(2018/10/11)
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- Pyrazolo [3, 4 - c] pyridine - 7 - ketone compound and use thereof
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Belonging to the technical field of medicine, the invention relates to a 4, 5-dihydro-1H-pyrazolo[3, 4-c]pyridine-7-one containing derivative shown as general formula I, and pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein the substituents A, R1 and R2 have meanings given in the specification. The preparation also relates to a preparation method of the general formula I compound and its pharmaceutically acceptable salt or prodrug, medicinal compositions containing the compound and application of the compound as an Xa factor inhibitor, especially application in preparation of drugs for treatment and/or prevention of thromboembolic diseases. (formula I).
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Paragraph 0197; 0238; 0249; 0250
(2017/09/01)
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- Supported Gold Nanoparticles for Efficient α-Oxygenation of Secondary and Tertiary Amines into Amides
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Although the α-oxygenation of amines is a highly attractive method for the synthesis of amides, efficient catalysts suited to a wide range of secondary and tertiary alkyl amines using O2as the terminal oxidant have no precedent. This report describes a novel, green α-oxygenation of a wide range of linear and cyclic secondary and tertiary amines mediated by gold nanoparticles supported on alumina (Au/Al2O3). The observed catalysis was truly heterogeneous, and the catalyst could be reused. The present α-oxygenation utilizes O2as the terminal oxidant and water as the oxygen atom source of amides. The method generates water as the only theoretical by-product, which highlights the environmentally benign nature of the present reaction. Additionally, the present α-oxygenation provides a convenient method for the synthesis of18O-labeled amides using H218O as the oxygen source.
- Jin, Xiongjie,Kataoka, Kengo,Yatabe, Takafumi,Yamaguchi, Kazuya,Mizuno, Noritaka
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supporting information
p. 7212 - 7217
(2016/07/06)
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- Iron(II) pincer-catalyzed synthesis of lactones and lactams through a versatile dehydrogenative domino sequence
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The synthesis of lactones and lactams by using iron(II) pincer-catalyzed dehydrogenative methodology was developed. Starting from 1,n-diols or 1,n-amino alcohols, this domino transformation takes place through initial dehydrogenation of the substrates, subsequent intramolecular cyclization, and final oxidation to afford the desired products in good yields. The ability to access heterocycles of different sizes makes this protocol especially versatile, in which two consecutive oxidation reactions are performed without requiring an external oxidant. In this paper, we report the application of the Fe-MACHO-BH complex [carbonylhydrido(tetrahydroborato)[bis(2-diisopropylphosphinoethyl)amino]iron(II)] in this atom-efficient and environmentally benign process, for which molecular hydrogen is formed as the only stoichiometric side product. Just a little pinch: The iron(II) pincer-catalyzed synthesis of lactones and lactams from easily available 1,n-diols and 1,n-amino alcohols is explored. The use of a nontoxic metal as well as the generation of molecular hydrogen as the only stoichiometric byproduct makes this method a highly atom-efficient and environmentally benign process.
- Pea-Lpez, Miguel,Neumann, Helfried,Beller, Matthias
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p. 865 - 871
(2015/03/14)
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- Construction of tertiary chiral centers by Pd-catalyzed asymmetric allylic alkylation of prochiral enolate equivalents
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Abstract The palladium-catalyzed decarboxylative allylic alkylation of enol carbonates derived from lactams and ketones is described. Employing these substrates with an electronically tuned Pd catalyst system trisubstituted chiral centers are produced. These stereocenters have been previously challenging to achieve using Pd complex/chiral P-N ligand systems.
- Kita, Yusuke,Numajiri, Yoshitaka,Okamoto, Noriko,Stoltz, Brian M.
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supporting information
p. 6349 - 6353
(2015/08/18)
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- HETEROARYL SULFONAMIDE COMPOUND OR SALT THEREOF
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PROBLEM TO BE SOLVED: To provide a novel herbicide. SOLUTION: The present invention provides a heteroaryl sulfonamide compound of the general formula (I) or a salt thereof, and a herbicide containing the compound as an active ingredient. [In the formula, A is O, S, SO, SO2 or CR8R9; W is O or S; Z is O, S or CR10R11; m and n are 0, 1 or 2 and satisfy 0≤n+m≤3; q is 0, 1, or 2; R1 is halo C1-C6 alkyl; R2 is H or C1-C12 alkoxycarbonyl; R3 is a halogen atom, optionally halo-substituted C1-C6 alkyl, C2-C6 alkenyl, alkynyl, C3-C6 cycloalkyl, C1-C6 alkylsulfonyl, or the like.] COPYRIGHT: (C)2015,JPOandINPIT
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Paragraph 0097
(2016/10/08)
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- Oxidant-free conversion of cyclic amines to lactams and H2 using water as the oxygen atom source
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Direct conversion of cyclic amines to lactams utilizing water as the only reagent is catalyzed by pincer complex 2. In contrast to previously known methods of amine-to-amide conversion, this reaction occurs in the absence of oxidants and is accompanied by liberation of H2, with water serving as a source of oxygen atom. Formation of a cyclic hemiaminal intermediate plays a key role in enabling such reactivity. This represents an unprecedented, conceptually new type of amide formation reaction directly from amines and water under oxidant-free conditions.
- Khusnutdinova, Julia R.,Ben-David, Yehoshoa,Milstein, David
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supporting information
p. 2998 - 3001
(2014/03/21)
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- Chemoselective conversion of α-unbranched aldehydes to amides, esters, and carboxylic acids by NHC-catalysis
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Depending on the N-heterocyclic carbene catalyst utilized, α-unbranched aldehydes selectively provided amides, esters, or carboxylic acids through oxidation by NCS. The α-unbranched aldehyde underwent these reactions chemoselectively in the presence of an aromatic or α-branched aldehyde.
- Kuwano, Satoru,Harada, Shingo,Oriez, Raphael,Yamada, Ken-Ichi
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experimental part
p. 145 - 147
(2012/01/12)
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- INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
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Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
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Page/Page column 35
(2012/01/03)
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- FACTOR XA INHIBITORS
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The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 24
(2008/06/13)
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- BICYCLIC 6-ALKYLIDENE-PENEM B-LACTAMASE INHIBITORS AND β-LACTAM ANTIBIOTIC COMBINATION: A BROAD SPECTRUM ANTIBIOTIC
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The present invention provides a β-lactam antibiotic such as cefepime and a compound of formula (I), pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
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Page/Page column 36
(2008/06/13)
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- UREAS AS FACTOR XA INHIBITORS
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The present invention is directed to compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 98-99
(2010/11/08)
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- THIOUREAS AS FACTOR Xa INHIBITORS
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The present invention is directed to compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 43
(2010/11/08)
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- TETRAHYDROISOQUINOLINES AS FACTOR XA INHIBITORS
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The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 44
(2008/06/13)
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- Osmium(VIII)-catalyzed oxidation of some cyclic amines by potassium hexacyanoferrate(III) in alkaline media: A kinetics and mechanistic study
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Reactions of morpholine, piperidine, and piperazine with Os(VIII) -catalyzed hexacyanoferrate(III) in alkaline media to produce the corresponding lactam have been studied at constant temperature and ionic strength. The reactions followed first-order kinetics with respect to [amine] and [Os(VIII)] but were independent of [Fe(CN)63-] and [OH-]. The effects of introduced electrolytes, potassium hexacyanoferrate(II), relative permitivity, and temperature have also been studied. A mechanism accounting for these results has been proposed.
- Al-Subu,Jondi,Amer,Hannoun,Musmar
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p. 478 - 484
(2007/10/03)
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- Bleaching compositions and additives comprising bleach activators having alpha-modified lactam leaving-groups
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Improved cleaning and/or bleaching compositions including fabric laundry and bleaching compositions, automatic dishwashing compositions, hard surface cleaners, bleach additives and the like, suitable for domestic use, comprising improved bleach activators having particular alpha-modified lactam leaving groups leading to improved in-use performance of bleaching agents such as perborate even under wash conditions less alkaline than those typically encountered or when hydrogen peroxide source is at low levels in a cleaning operation. A preferred class of activators are N-acyl-3-morpholinone compounds with benzoyl being a preferred acyl group and N-Benzoyl-3-oxomorpholine being a highly preferred activator.
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- Diphosphonic acid compounds and use for calcium metabolism disorders
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The present invention provides compounds of the formula: STR1 The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them useful in treatment and prophylaxis of disorders of calcium metabolism.
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