- Synthesis, characterization and DNA-binding studies of 1-cyclohexyl-3-tosylurea and its Ni(II), and Cd(II) complexes
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1-Cyclohexyl-3-tosylurea (HL) and its two complexes, ML2·2H2O [M{double bond, long}Ni(1), and Cd(2)], have been synthesized and characterized on the basis of elemental analyses, molar conductivities, IR spectra and thermal analyses. In addition, the DNA-binding properties of the ligand and the two complexes have been investigated by electronic absorption, fluorescence, CD spectroscopy and viscosity measurements. The experiment results suggest that the ligand and its two complexes bind to DNA via a groove binding mode, and the binding affinity of the complex 2 is higher than that of the complex 1 and the ligand.
- Xi, Pin-xian,Xu, Zhi-hong,Liu, Xiao-hui,Cheng, Feng-juan,Zeng, Zheng-zhi
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- Synthesis, characterization, antioxidant activity, and DNA-binding studies of 1-cyclohexyl-3-tosylurea and its Nd(III), Eu(III) complexes
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A new ligand, 1-cyclohexyl-3-tosylurea (H2L), was prepared by condensation ethyl N-(3-tossulfonyl) carbamate and cyclohexanamine. Its two lanthanide(III) complexes, Ln(H2L)3·3NO3 [Ln=Nd (1), and Eu (2)], have been synthesized and characterized on the base of element analyses, ESI-MS, molar conductivities, IR spectra and thermogravimetry/differential thermal analysis (TG-DTA). In addition, the DNA-binding properties of the ligand and its complexes have been investigated by electronic absorption spectroscopy, fluorescence spectroscopy, circular dichroic (CD) spectroscopy and viscosity measurements. The experiment results suggest that the ligand and its two complexes bind to DNA via a groove binding mode, and the binding affinity of the complex 2 is higher than that of the complex 1 and the ligand. Furthermore, the antioxidant activity (superoxide and hydroxyl radical) of the ligand and its metal complexes was determined by using spectrophotometer methods in vitro. These complexes were found to possess potent antioxidant activity and be better than standard antioxidants like vitamin C and mannitol. In particular, complex 2 displayed excellent activity on the superoxide and hydroxyl radical.
- Xi, Pin-Xian,Xu, Zhi-Hong,Liu, Xiao-Hui,Chen, Feng-Juan,Huang, Liang,Zeng, Zheng-Zhi
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- PROCESS FOR PREPARATION OF GRAPIPRANT
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The invention relates to process for the preparation of grapiprant and its intermediates thereof. The invention also relates to grapiprant having a purity 98% or more and compounds of Formula (A), (B), (C) and (D) in an amount of 0.5 or less, relative to grapiprant, by area percentage of HPLC. The invention also relates to an amorphous form of grapiprant and process for preparation thereof.
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Paragraph 0134-0135
(2021/03/19)
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- A sulfonyl urea, sulfonamide ethyl ester preparation method of compound (by machine translation)
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The description relates to a compound of formula (I) compound of the preparation method, wherein formula (II) with a compound represented by formula (III) as shown in the catalysis of palladium catalyst, under a carbon monoxide atmosphere, reacts in a solvent to obtain the compound. The invention related to the method of the reaction do not require strict-free conditions, does not need a high pressure carbon monoxide atmosphere, convenient and simple to operate, to a functional group and has very high power density and universality, the catalyst consumption is very small, the cost of reaction is very low, and can be widely used for preparing sulfonyl urea compound. R1 - SO2 - NH - CO - X (R3 )n - R2 (I) R1 - SO2 - R4 (II) HX (R3 )n - R2 (III) wherein X is O or N; n is 0 or 1; when X is when O, n=0; when X is when N, n=1; R1 Selected from aryl, heteroaryl, alkyl, alkenyl or alkynyl; R2 Selected from aryl, heteroaryl, alkyl, alkenyl or alkynyl; R3 Is selected from H, R2 , Or R3 And R2 A ring of connection; R4 For N3 Or a halogen atom; when R4 For nails halogen original, system also comprises a sodium azide. (by machine translation)
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Paragraph 0094; 0100-0104; 0110-0115
(2017/08/02)
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- Product-Derived Bimetallic Palladium Complex Catalyzes Direct Carbonylation of Sulfonylazides
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A novel product-derived bimetallic palladium complex catalyzes a sulfonylazide-transfer reaction with the σ-donor/π-acceptor ligand CO, and is advantageous given its broad substrate scope, high efficiency, and mild reaction conditions (atmospheric pressure of CO at room temperature). This methodology provides a new approach to sulfonylureas, which are present in both pharmaceuticals and agrochemicals. The synthesis of Glibenclamide on a gram scale further revealed the practical utility of this procedure. Mechanistically, the generation of a bridged bimetallic palladium species derived from the product sulfonylurea is disclosed as the crucial step for this catalytic cycle.
- Zhao, Jin,Li, Zongyang,Song, Shaole,Wang, Ming-An,Fu, Bin,Zhang, Zhenhua
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p. 5545 - 5549
(2016/05/09)
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- Rapid and straightforward transesterification of sulfonyl carbamates
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A fast and convenient method for the alkoxy exchange of sulfonyl carbamates by simply heating in a chosen alkyl alcohol is described. No catalysts or additives are required. Microwave heating at 100-120 °C for 20-60 min resulted in good to excellent yields (53-93%) of alkyl (arylsulfonyl)carbamates where the alkyl part originates from the alcohol solvent. The developed protocol was applied to the synthesis of an angiotensin II type 2 receptor (AT2R) ligand.
- Isaksson, Rebecka,Kumpi?a, Ilze,Larhed, Mats,Wannberg, Johan
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p. 1476 - 1478
(2016/03/12)
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- Green and practical synthesis of carbamates from ureas and organic carbonates
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A practical method for the synthesis of carbamates from ureas and organic carbonates was developed with 100% atom economy using La2O 3/SiO2 as catalyst without any additional solvent. The scope of the protocol is demonstrated in the synthesis of 14 carbamates with various functional groups in excellent yields (76-95%).
- Guo, Xiaoguang,Shang, Jianpeng,Li, Jian,Wang, Liguo,Ma, Yubo,Shi, Feng,Deng, Youquan
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experimental part
p. 1102 - 1111
(2011/05/02)
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- Use of an arylsulphonylurethane as film forming resin in nitrocellulose nail varnishes, new arylsulphonylurethanes and new nitrocellulose nail varnishes
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The present invention lies in the field of nitrocellulose nail varnishes and its subject is the use of an arylsulphonylurethane as film forming resin in these varnishes, which makes it possible in particular to avoid the release of formaldehyde, a carcinogenic compound which is formed when an arylsulphonamide-formaldehyde resin is employed. Another subject of the invention is new poly(arylsulphonylurethanes) containing from 2 to 5 arylsulphonylurethane groups and possessing a molecular mass of between 450 and 1500.
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- Synthesis of N-Acyl-, N-Sulfonyl-, and N-Phosphinylphospha-λ5-azenes by a Redox-Condensation Reaction Using Amides, Triphenylphosphine, and Diethyl Azodicarboxylate
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The reaction of phosphines and amides with diethyl azodicarboxylate (DAD) produced phospha-λ5-azenes.Thus aromatic amides and those aliphathic amides with electron-withdrawing substituents gave N-acyl-P,P,P-triphenylphospha-λ5-azenes (5) when triphenylphosphine (TPP) was employed.Both aryl- and alkylsulfonamides reacted with TPP and DAD to produce the N-sulfonylphospha-λ5-azenes (9).Diphenylphosphinamide (10) and ethyl carbamate (12) also produced the respective phosphazenes (11 and 13) with TPP and DAD.Secondary carboxamides and sulfonamides did not react with TPP and DAD.The reaction of triethyl phosphite with sulfonamides in the presence of DAD produced the phosphorimidates (20) in an analogous reaction, along with the corresponding N,N-diethylsulfonamides and the deethylated adduct of triethyl phosphite and DAD (23).Triethyl phosphite-DAD failed, however, to give a phosphorimidate with carboxamides but gave, instead, the rearranged adduct of DAD and triethyl phosphite (19).Tris(dimethylamino)phosphine reacted with sulfonamides and DAD but the products were the corresponding ethyl N-sulfonylcarbamates (26) rather than the phosphazenes.Tris(dimethylamino)phosphine reacted with azodicarbonamide (a molecule which contains both the azo and carboxamide groups) with the production of N,N-dimethylurea, again without formation of the phosphazene.Finally, the reaction of triphenylarsine with benzenesulfonamide and DAD produced N-(phenylsulfonyl)triphenylarsa-λ5-azene (30) but triphenylstibene with DAD and benzenesulfonamide only gave triphenylstibene oxide.Mechanistic possibilities for these reactions are also discussed.
- Bittner, Shmuel,Assaf, Yonit,Krief, Penina,Pomerantz, Martin,Ziemnicka, Barbara T.,Smith, Christina G.
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p. 1712 - 1718
(2007/10/02)
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- N-arylsulfonyl carbamates
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The present invention relates to amine, alkali metal and alkaline earth metal salts of N-benzene sulfonyl carbamic acid esters and to lower alkenyl N-benzene sulfonyl carbamates. These compounds are useful as herbicides.
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