- Modular Synthesis of Carbon-Substituted Furoxans via Radical Addition Pathway. Useful Tool for Transformation of Aliphatic Carboxylic Acids Based on "build-and-Scrap" Strategy
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Utilizing radical chemistry, a new general C-C bond formation on the furoxan ring was developed. By taking advantage of the lability of furoxans, a wide variety of transformation of the synthesized furoxans have been demonstrated. Thus, this developed methodology enabled not only the modular synthesis of furoxans but also short-step transformations of carboxylic acids to a broad range of functional groups.
- Matsubara, Ryosuke,Kim, Hojin,Sakaguchi, Takaya,Xie, Weibin,Zhao, Xufeng,Nagoshi, Yuto,Wang, Chaoyu,Tateiwa, Masahiro,Ando, Akihiro,Hayashi, Masahiko,Yamanaka, Masahiro,Tsuneda, Takao
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p. 1182 - 1187
(2020/02/15)
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- Autolysis multi-functional liposome and application thereof
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The invention relates to an autolysis multi-functional liposome and an application thereof. A preparation method comprises the steps of sequentially introducing a nitric oxide donor, polyethylene glycol and super paramagnetism ferroferric oxide nanoparticles to amino ends of distearoyl-phosphatidylethanolamine so as to obtain magnetic targeted phospholipid of a NO donor bridge chain. The magnetictargeted phospholipid of a NO donor bridge chain disclosed by the invention can be used as main components and cooperate with other auxiliary materials of distearoyl phosphatidylcholine, cholesterol and the like to prepare nanometer liposome. The liposome disclosed by the invention can be used for packing antitumor drugs of adriamycin and the like. The obtained drug delivery system is favorable instability under the physiological condition, and besides, under the condition of external magnetic field, the drug delivery system can be enriched in a magnetic field region, so that magnetism targeting can be realized; and the NO donor can split to release No molecules under the action of promotion factors of glutathione and the like, so that improvement of antineoplastic activity and overcomingof tumor drug tolerance are facilitated, the nanometer liposome can be disintegrated, and drugs are released and loaded. The drug release efficiency of the drug delivery system is improved, and the tumor treatment effect can be increased.
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- Synthesis and antioxidant activity of bis unsaturated sulfones, bis pyrroles, and bis pyrazoles
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The Michael acceptor 1,4-bis-(E)-2-(arylsulfonylvinyl)benzene was exploited to prepare a new series of bis heterocycles-(1,4-phenylene)bis(arylsulfonylpyrrole) and (1,4-phenylene)bis(arylsulfonyl pyrazole). All of the compounds were tested for antioxidant activity. Amongst the tested compounds, 1,4-bis-(E)-2-(arylsulfonylvinyl)benzene (5) was found to be the best potential antioxidant agent.
- Lavanya,Prakash, T. Bhanu,Sravya,Padmavathi,Padmaja
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p. 8815 - 8828
(2015/10/28)
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- A facile and effective synthesis of 2-azetidinones via phosphonitrilic chloride
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The Staudinger reaction of imines to β-lactams was successfully achieved with substituted acetic acid and phosphonitrilic chloride in one-pot under mild conditions. Several types of β-lactams, especially 3-electron-withdrawing group β-lactams, can be synthesized by this versatile and efficient method in good to excellent yields. This method is simple, clean, and the by-products were removed by simple aqueous work-up. The effects of solvents, molar ratio of reagent, and the temperature were considered.
- Zarei, Maaroof
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p. 6620 - 6626
(2013/07/26)
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- Solid phase synthesis of 3-toluenesulfonylglutarimides
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A novel route for the synthesis of 3-toluenesulfonylglutarimides on a solid support is described. The cyclization step involves stepwise [3+3] strategy of Rink Amide resin bound onto an α-toluenesulfonyl group with various α,β-unsaturated esters.
- Chang, Meng-Yang,Lin, Kuo-Ging,Chen, Shui-Tein,Chang, Nein-Chen
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p. 795 - 797
(2007/10/03)
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- The Preparation and Some Reactions of 2-(Arylsulfonyl)vinamidinium Salts
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The preparation of novel 2-(arylsulfonyl)vinamidinium salts is described.The reactions of these materials with amidines, hydrazine, hydroxylamine, sodium borohydride, and Grignard reagents are presented along with an evaluation of their chemical behavior as compared to the 2-arylvinamidinium salts.
- Gupton, John T.,Riesinger, Steve W.,Shah, Ajit S.,Gall, John E.,Bevirt, Kathy M.
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p. 976 - 980
(2007/10/02)
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- Carboxylic acid derivatives, processes for the preparation thereof, the use thereof, and pharmaceutical compositions which contain these compounds
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This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
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- Mass spectra of arylsulphonylacetic acids and correlation of fragment ions with substituent constants
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The mass spectral studies of arylsulphonylacetic acids reveal that the skeletal rearrangement via aryl-oxygen bond formation is predominant with a weak competing alkyl migration.A linear correlation is obtained between the intensities of + ions, i.e. +> and the Hammett substituent constants.
- Srinavasan, C.,Ganesan, P. K.,Shunmugasundaram, A.,Vairamani, M.
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p. 141 - 145
(2007/10/02)
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- SYNTHESIS OF ORGANOSULFONYLACETIC ACID
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Alkylsulfonylacetic acids and their esters were obtained by the alcoholysis of alkyl β,β-dichlorovinyl sulfones and the oxidation of alkylthioacetic acids.Arylsulfonylacetic acids were synthesized by the reaction of sodium arenesulfinates with monochloroacetic acid.The optimum conditions for the reaction were obtained.Arylsulfonylacetic esters were obtained by the reaction of monochloroacetic esters with sodium arenesulfinate in DMFA, and their hydrolysis led to the corresponding acids with yields of 65-98percent.Dichloroacetic estersreacts with arenesulfinates, forming di(arylsulfonyl)acetic esters.
- Mirskova, A.N.,Kryukova, Yu.I.,Levkovskaya, G.G.,Guseva, S.A.,Voronkov, M.G.
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p. 545 - 550
(2007/10/02)
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- MODERN FRIEDEL-CRAFTS CHEMISTRY. XI. CYCLIZATION OF ARYL HALOALKYL SULFONES, ARYLSULFONYLACYL CHLORIDES AND THEIR CORRESPONDING SULFIDES
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The sulfone group deactivation for cyclialkylation and cycliacylation reactions in the presence of Friedel-Crafts catalysts was demonstrated in a number of aryl chloroalkylsulfones (1-8) and arylsulfonylacyl chlorides (17a-22a), respectively.As expected, the corresponding arylchloroalkyl sulfides (9-16) and arylmercaptoacyl chlorides (13a-28a) underwent ring-closure reaction in most cases under the same conditions.The ease of cyclization was governed by the ring size, the stability of the attacking carbocation and the nucleophilicity of the aryl moiety.Also, the behaviour of benzyl sulfones (29, 31a, and 32a) and sulfides (33, 34a and 36a) was inconsistent.Noteworthy, the Friedel-Crafts cyclization reaction is thus considered an accessible method for the synthesis of compounds 37-41 and 45, 51.
- Abdel-Wahab, Aboel-Magd A.,El-Khawaga, Ahmed M.,El-Zohry, Maher F.,Khalaf, Ali A.
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