- Combinatorial synthesis of dihydropyridone libraries and their derivatives
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Polymer-supported quench methodology has been used for parallel purification of combinatorial libraries of dihydropyridones and their derivatives. The dihydropyridone scaffold was assembled via a solution phase Lewis acid catalyzed, hetero-Diels-Alder reaction. Further modifications allow for the rapid generation of subsequent aminopiperidine and acylaminopiperidine libraries utilizing a library from library approach.
- Creswell, Mark W.,Bolton, Gary L.,Hodges, John C.,Meppen, Malte
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- Spectrophotometric studies on the inclusion formation of β-cyclodextrin with 3,4-(methylenedioxyphenyl) benzylideneaniline
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Complexation of β-cyclodextrin with 3,4-(methylenedioxyphenyl) benzylideneaniline has been studied in aqueous solution by means of spectrophotometry. It was observed that the complexation attains equilibrium very slowly. The equilibrium constant of the 1:
- Chen, Jian,Sun, Dezhi,Feng, Changgen
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- A Highly Selective Manganese-Catalyzed Synthesis of Imines under Phosphine-Free Conditions
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An efficient and highly selective phosphine-free NN-manganese(I) complex catalyst system was developed for the acceptorless dehydrogenative coupling of alcohols with amines to form imines. The coupling reactions underwent at 3 mol % catalyst loading, and a large range of alcohols and amines with diverse functional groups was applied, including challenging diol and diamine. The target imine products were obtained in good to excellent yields. The present work provides an alternative method to construct highly active nonprecious metal complex catalysts based on phosphine-free ligands.
- Chai, Huining,Yu, Kun,Liu, Bo,Tan, Weiqiang,Zhang, Guangyao
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p. 217 - 226
(2020/01/31)
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- Design and Synthesis of 5-Substituted Benzo[d][1,3]dioxole Derivatives as Potent Anticonvulsant Agents
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A series of 5-substituted benzo[d][1,3]dioxole derivatives was designed, synthesized, and tested for anticonvulsant activity using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens. Neurotoxicity was determined by rotarod test. In the preliminary screening, six compounds, 3a, 3c, 3d, and 4d–f, showed promising anticonvulsant activities in the MES model, and compounds 4c and 4d exhibited full protection against seizures at doses of 300 mg/kg in the scPTZ model. Among the synthesized compounds, 3c as the most active compound showed high protection against the MES-induced seizures with an ED50 value of 9.8 mg/kg and a TD50 value of 229.4 mg/kg after intraperitoneal injection into mice, thus providing compound 3c with a high protective index (TD50/ED50) of 23.4 comparable to those of reference antiepileptic drugs.
- Dong, Shiyang,Wang, Tiantian,Hu, Chundi,Chen, Xiaodong,Jin, Yi,Wang, Zengtao
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- NOVEL PIPERINE DERIVATIVES AND USES THEREOF
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The present invention provides novel piperine derivatives. The present pharmaceutical or food composition containing a piperine derivative as an active ingredient is very effective in preventing or treating metabolic diseases including obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome. Piperine derivatives of the present invention useful as pharmaceuticals compositions or functional food compositions has therapeutic efficacies for metabolic syndrome selected from the group consisting of obesity, diabetes, hyperlipidemia, fatty liver and insulin resistance syndrome, and also suppress the differentiation of progenitor cells and reduce the accumulation of triglycerides.
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Paragraph 0095; 0096
(2015/01/06)
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- NOVEL PIPERINE DERIVATIVE AND USE THEREFOR
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The present invention provides novel piperine derivatives. The present pharmaceutical or food composition containing a piperine derivative as an active ingredient is very effective in preventing or treating metabolic diseases including obesity, diabetes,
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Paragraph 0079; 0080
(2015/01/16)
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- Synthesis of cucurbitine derivatives: facile straightforward approach to methyl 3-amino-4-aryl-1-methylpyrrolydine-3-carboxylates
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A general three- or four-step synthesis of cis- and trans-substituted cucurbitine (3-aminopyrrolidine-3-carboxylic acid) derivatives from methyl 2-nitroacetate is reported. The first step utilizes a Knoevenagel condensation with five different aromatic imines or their corresponding aldehydes to form (Z/E)-mixtures of α-nitro acrylates. The second step gives rise to the pyrrolidine-core structures of the title compounds by a 1,3-dipolar cycloaddition reaction using an azomethine ylide. The last step consists of reduction of the nitro group to yield both diastereoisomers of the corresponding 4-aryl cucurbitine methyl esters.
- Blanco-Ania, Daniel,Hermkens, Pedro H.H.,Sliedregt, Leo A.J.M.,Scheeren, Hans W.,Rutjes, Floris P.J.T.
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supporting information; experimental part
p. 5393 - 5401
(2009/10/17)
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- Fast and efficient synthesis of pyrano[3,2-c]quinolines catalyzed by niobium(V) chloride
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A highly efficient two-step method for the synthesis of pyranoquinoline derivatives from imino-Diels-Alder reactions between aldimines and 3,4-dihydro-2H-pyran using niobium(V) chloride as catalyst under mild conditions is described. Georg Thieme Verlag Stuttgart.
- Da Silva-Filho, Luiz Carlos,Lacerda Jr., Valdemar,Constantino, Mauricio Gomes,Da Silva, Gil Valdo Jose
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experimental part
p. 2527 - 2536
(2009/04/04)
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- Eco-friendly synthesis of imines by ultrasound irradiation
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A series of imines was synthesized by an ultrasound-assisted reaction of aldehydes and primary amines using silica as the promoter. Products were obtained in high yields even in large scale synthesis.
- Guzen, Karla P.,Guarezemini, Alexandre S.,órf?o, Aline T.G.,Cella, Rodrigo,Pereira, Claudio M.P.,Stefani, Hélio A.
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p. 1845 - 1848
(2008/02/05)
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- Molecular sieves in ionic liquids as an efficient and recyclable medium for the synthesis of imines
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A great variety of imines were efficiently isolated in high yields from the reaction of aldehydes and amines in ionic liquids. The ionic liquids could be recovered and reused for at least five cycles without loss in the yields being a useful alternative to dichloromethane or diethyl ether, which are the commonly used solvents for this reaction.
- Andrade, Carlos Kleber Z.,Takada, Sayuri Cristina S.,Magalh?es Alves, Luana,Petrocchi Rodrigues, Juliana,Suarez, Paulo Anselmo Z.,Brand?o, Rodrigo Fleury,Soares, Valério Cassiano D.
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p. 2135 - 2138
(2007/10/03)
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