- Compound with anti-aging and discoloration-resistant effects and preparation method thereof
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The invention provides a compound with anti-aging and discoloration-resistant effects and a preparation method thereof. The compound has a structure shown as a formula (I), and in the formula, R, R1 and R2 are defined in the description. Compared with an
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Paragraph 0080-0082; 0090-0092
(2021/05/08)
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- Stable isotope labeled atrazine-d5 and synthesis method thereof
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The invention discloses stable isotope labeled atrazine and a synthetic method thereof. The stable isotope labeled ethyl-d5-amine hydrochloride serves as a stable isotope labeling source, firstly, 2,4, 6-trichloro-1, 3, 5-triazine reacts with isopropylamine to obtain 2, 4-dichloro-6-isopropylamino-1, 3, 5-triazine, and then reaction with stable isotope labeled ethyl-d5-amine hydrochloride is carried out to obtain a stable isotope labeled atrazine-d5 product. The used stable isotope labeling raw material is ethyl-d5-amine hydrochloride, the source is easy to obtain, the price is low, the synthesis process is simple, the product is easy to separate and purify, the chemical purity and isotope abundance of the obtained product both reach 98% or above, and the related requirements of a standard reagent for quantitatively detecting the content of atrazine are met.
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Paragraph 0025-0029
(2021/01/04)
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- Continuous production method of multi-kettle serial triazine herbicide
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The invention relates to a continuous production method of a multi-kettle serial triazine herbicide. A metered cyanuric chloride solution is pre-cooled and mixed with alkylamine R1 in a mixer to entera first-stage reaction kettle, continuous discharging is conducted, after a heat exchanger is passed, the cyanuric chloride solution is neutralized with alkali in the mixer and enters a first-stage neutralization kettle, after a reaction is completed, the cyanuric chloride solution passes through a continuous water separator and the heat exchanger and is mixed with alkylamine R2 in the mixer to enter a second-stage reaction kettle, the continuous discharging is conducted, after the cyanuric chloride solution passes through the heat exchanger, the cyanuric chloride solution is mixed with the alkali in the mixer to enter a second-stage neutralization kettle, after the neutralization, a aqueous phase is separated by a continuous layerer, a solvent is removed, and drying is conducted to obtain a triazine product. The production method has the advantages of high productivity, good production stability, high efficiency, high product quality and the like, is particularly suitable for technical transformation of existing production enterprises, has a low transformation cost, basically does not add novel reaction equipment, and is easily mastered by existing enterprises.
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Paragraph 0090-0094
(2019/05/04)
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- Synthesis of new 5-aza-isosteres of guanine containing aryl and hetaryl substituents on the 1,2,4-triazole ring
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The oxidative cyclization of 4-amino-substituted 6-arylidene(hetarylmethylidene)hydrazinyl-1,3,5-triazin-2-ones with lead(IV) tetraacetate proceeds via a Dimroth-type rearrangement to give 5-amino-substituted 2-aryl(hetaryl)-1,2,4-triazolo[1,5-a]-1,3,5-tr
- Zavodskaya, Anna V.,Bakharev, Vladimir V.,Parfenov, Victor E.,Gidaspov, Alexander A.,Slepukhin, Pavel A.,Isenov, Maksim L.,Eltsov, Oleg S.
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p. 1103 - 1106
(2015/02/19)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
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Page/Page column 135
(2013/07/19)
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- Synthesis of 4-amino-6-chloro-1,3,5-triazin-2(1H)-ones
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Conditions for selective substitution for one chlorine atom in 2-(R,R-amino)-4,6-dichloro-1,3,5-triazines with a hydroxide ion were elaborated. Spectral and calculation methods showed that the products formed are in the lactam form, i.e., have the structure of 4-chloro-6-(R,R- amino)-1,3,5-triazin-2(1H)-ones.
- Bakharev,Gidaspov,Parfenov,Ulyankina,Zavodskaya,Selezneva,Suponitskii,Sheremetev
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- Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT)
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The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. To identify selective inhibitors of ADAMTS-5, we employed encoded library technology (ELT), which enables affinity selection of small molecule binders from complex mixtures by DNA tagging. Selection of ADAMTS-5 against a four-billion member ELT library led to a novel inhibitor scaffold not containing a classical zinc-binding functionality. One exemplar, (R)-N-((1-(4-(but-3-en-1-ylamino)-6-(((2-(thiophen-2-yl)thiazol-4-yl)methyl) amino)-1,3,5-triazin-2-yl)pyrrolidin-2-yl)methyl)-4-propylbenzenesulfona-mide (8), inhibited ADAMTS-5 with IC50 = 30 nM, showing >50-fold selectivity against ADAMTS-4 and >1000-fold selectivity against ADAMTS-1, ADAMTS-13, MMP-13, and TACE. Extensive SAR studies showed that potency and physicochemical properties of the scaffold could be further improved. Furthermore, in a human osteoarthritis cartilage explant study, compounds 8 and 15f inhibited aggrecanase-mediated 374ARGS neoepitope release from aggrecan and glycosaminoglycan in response to IL-1β/OSM stimulation. This study provides the first small molecule evidence for the critical role of ADAMTS-5 in human cartilage degradation.
- Deng, Hongfeng,O'Keefe, Heather,Davie, Christopher P.,Lind, Kenneth E.,Acharya, Raksha A.,Franklin, G. Joseph,Larkin, Jonathan,Matico, Rosalie,Neeb, Michael,Thompson, Monique M.,Lohr, Thomas,Gross, Jeffrey W.,Centrella, Paolo A.,O'Donovan, Gary K.,Bedard, Katie L.,Van Vloten, Kurt,Mataruse, Sibongile,Skinner, Steven R.,Belyanskaya, Svetlana L.,Carpenter, Tiffany Y.,Shearer, Todd W.,Clark, Matthew A.,Cuozzo, John W.,Arico-Muendel, Christopher C.,Morgan, Barry A.
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p. 7061 - 7079
(2012/11/07)
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- Design, synthesis, and biological activities of arylmethylamine substituted chlorotriazine and methylthiotriazine compounds
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Heterocyclic rings were introduced into the core structure of s-triazine to design and synthesize a series of novel triazines containing arylmethylamino moieties. These compounds were characterized by using spectroscopic methods and elemental analysis. Their herbicidal, insecticidal, fungicidal, and antitumor activities were evaluated. Most of these compounds exhibited good herbicidal activity, especially against the dicotyledonous weeds, and compound F8 was almost at the same level as the control compound atrazine. Their structure-activity relationships were discussed. At the same time, some triazines had interesting fungicidal and insecticidal activities, of which F4 exhibited 100% efficacy against Puccinia triticina even at 20 ppm, and F5 showed Lepidopteran-specific activity in both leaf-piece and artificial diet assays. Moreover, these compounds showed antitumor activities against leukemia HL-60 cell line and lung adenocarcinoma A-549 cell line.
- Zhao, Huaping,Liu, Yuxiu,Cui, Zhipeng,Beattie, David,Gu, Yucheng,Wang, Qingmin
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experimental part
p. 11711 - 11717
(2012/04/17)
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- Identification and optimization of inhibitors of trypanosomal cysteine proteases: Cruzain, rhodesain, and TbCatB
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Trypanosoma cruzi and Trypanosoma brucei are parasites that cause Chagas' disease and African sleeping sickness, respectively. Both parasites rely on essential cysteine proteases for survival: cruzain for T. cruzi and TbCatB/rhodesain for T. brucei. A rec
- Mott, Bryan T.,Ferreira, Rafaela S.,Simeonov, Anton,Jadhav, Ajit,Ang, Kenny Kean-Hooi,Leister, William,Shen, Min,Silveira, Julia T.,Doyle, Patricia S.,Arkin, Michelle R.,McKerrow, James H.,Inglese, James,Austin, Christopher P.,Thomas, Craig J.,Shoichet, Brian K.,Maloney, David J.
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supporting information; experimental part
p. 52 - 60
(2010/04/29)
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- Evaluation of the carbonyl metallo immunoassay (CMIA) for the determination of traces of the herbicide atrazine
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The non-isotopic immunoassay (CMIA) was investigated for the quantification of the herbicide atrazine. This assay combines transition metal carbonyl complex and Fourier transform infrared spectroscopy. We describe the synthesis of three dicobalt hexacarbonyl tracers, derivatives of atrazine. Their relative binding affinity towards two purified IgG fractions of polyclonal rabbit anti-sera (anti-atrazine and -simazine) was evaluated by ELISA and CMIA. The best tracer 9 (bearing the longest alkyl chain between atrazine aromatic ring and metal carbonyl complex) was used for further study by CMIA. Reproducible competitive standard curves were obtained by using anti-simazine antibodies in PBS buffer pH 7.4 with pre-incubation of various amounts of atrazine and antibodies for 1 h at 4 °C before addition of the tracer. This study demonstrates the feasability of using CMIA for pesticide determination, although the sensitivity of current CMIA format does not reach the 0.1 μg 1-1 level required by E.U.
- Fischer-Durand, Nathalie,Vessières, Anne,Heldt, Jan-Martin,le Bideau, Franck,Jaouen, Gérard
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- Evaluation and Optimisation of the Reagent Addition Sequence during the Synthesis of Atrazine (6-Chloro-N2-ethyl-N4-isopropyl-1,3, 5-triazine-2,4-diamine) Using Reaction Calorimetry
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The sequence of reagent addition and associated heats of reaction during the synthesis of the important herbicide atrazine (6-chloro-N 2-ethyl-N4-isopropyl-1,3,5-triazine-2,4-diamine) from cyanuric chloride, isopropylamine, and ethylamine have been investigated by means of calorimetric and analytical methods. Sodium hydroxide was used as proton scavenger in this procedure. The best addition sequence found was the concurrent addition of amine and NaOH, keeping the amine in slight excess at all times. Using this feed sequence, the reaction becomes feed-controlled, and provided that a proper level of mixing can be maintained in the reactor, a high degree of control over reaction selectivity is obtained.
- Barton, Benita,Gouws, Shawn,Schaefer, Melissa C.,Zeelie, Bernard
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p. 1071 - 1076
(2013/09/05)
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- Selective NPY (Y5) antagonists (triazines)
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This invention is directed to triazine derivatives which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
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Page column 17
(2010/01/30)
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- Triazine compounds
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The present invention discloses new herbicidally active triazine compounds of the formula STR1 wherein R represents hydrogen, C1 -C6 alkyl which is unsubstituted or substituted by cyano, hydroxy, C1 -C4 alkoxy, cyclopropyl, methylcyclopropyl, or a radical STR2 wherein R1 represents hydrogen or methyl X represents chlorine, methoxy, methylthio, azido or cyano and Y represents a halogen atom. These compounds are particularly useful for controlling weeds in crops of rice.
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- Process for the production of chloro-bis(alkylamino)-s-triazines
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The commercial method of preparing chloro-bis(alkylamino)-s-triazine by step-wise replacement of two chlorine atoms of cyanuric chloride by means of alkylamino groups in an alkaline medium comprising water and a liquid organic compound is improved by adding to the reaction product, upon completion of the second replacement step, or during or after the distillation of the organic compound, at least 0.5% by weight with respect to the weight of the chloro-bis(alkylamino)-s-triazine, of minerals chosen from the groups of montmorillonite, paligorskite, vermiculite and chlorite and having a base-exchange capacity of at least 10 milli-equivalents for each 100 grams of said solid, thus deactivating the unreacted alkylamine and the tris(alkylamino)-s-triazines present in the reaction product.
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- N-(2,4-dihalo-S-triazin-6-yl)-ureas and process for their manufacture
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A process for the manufacture of N-(2,4-dihalo-s-triazin-6-yl)-ureas of the formula SPC1 Wherein X represents halogen, R represents alkyl, aryl or hydrogen and Y represents hydrogen or the sulphonic acid group, which comprises reacting a dihalo-amino-s-triazine of the formula SPC2 Wherein X and R have the meanings assigned to them hereinbefore, with chloro-sulphonylisocyanate and hydrolysing the resulting reaction product. The compounds of the formula (1) are suitable as starting products for the manufacture of reactive dyes, fluorescent whiteners or agro - chemicals.
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