- COMPOUND USED AS AUTOPHAGY REGULATOR, AND PREPARATION METHOD THEREFOR AND USES THEREOF
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It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.
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Paragraph 0249-0250
(2020/07/07)
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- Preparation method of 2,3-dihydrobenzofuran
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The invention discloses a preparation method of 2,3-dihydrobenzofuran. The preparation method comprises the following steps: with phenol and 2-bromoacetaldehyde diethyl acetal as initial raw materials, carrying out condensing to obtain 2-phenoxyacetaldehyde diethyl acetal; carrying out cyclizing to obtain benzofuran; and finally, conducting hydrogenating to obtain 2,3-dihydrobenzofuran. The methodprovided by the invention can be used for preparing 2,3-dihydrobenzofuran, and has the advantages of easily available raw materials, mild reaction conditions, easy operation, good product quality, high yield, low cost, small environmental pollution and relatively high economic benefits.
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Paragraph 0027-0028
(2020/07/02)
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- Palladium-Catalyzed Regioselective C-2 Arylation of Benzofurans with N′-Acyl Arylhydrazines
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A novel ligand-free palladium-catalyzed C-2 arylation of benzofurans has been developed using N′-acyl arylhydrazines as the coupling partners and TEMPO as an oxidant. This protocol features a wide functional-group tolerance and highly regioselective products with good to excellent yields.
- Cao, Jun,Chen, Zi-Li,Li, Shu-Min,Zhu, Gao-Feng,Yang, Yuan-Yong,Wang, Cong,Chen, Wen-Zhang,Wang, Jian-Ta,Zhang, Ji-Quan,Tang, Lei
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supporting information
p. 2774 - 2779
(2018/06/21)
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- A Pincer Ruthenium Complex for Regioselective C-H Silylation of Heteroarenes
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A pincer Ru(II) catalyst for the highly efficient undirected silylation of O- and S-heteroarenes with (TMSO)2MeSiH and Et3SiH is described, producing heteroarylsilanes with exclusive C2-regioselectivity, good functional-group tolerance, and high turnover numbers (up to 1960). The synthetic utility of the silylated products is demonstrated by Pd-catalyzed Hiyama-Denmark cross-coupling under mild conditions. One-pot, two-step silylation and coupling procedures have been also developed.
- Fang, Huaquan,Guo, Le,Zhang, Yuxuan,Yao, Wubing,Huang, Zheng
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supporting information
p. 5624 - 5627
(2016/11/17)
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- Zeolite-catalyzed synthesis of 2,3-unsubstituted benzo[b]furans via the intramolecular cyclization of 2-aryloxyacetaldehyde acetals
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An efficient and environmentally benign heterogeneous catalytic process for the synthesis of 2,3-unsubstituted benzo[b]furans has been established via the intramolecular cyclization of 2-aryloxyacetaldehyde acetals. By utilizing tin-exchanged H-β zeolite (Sn-β) as catalyst, a wide range of functionalized 2,3-unsubstituted benzo[b]furans could be prepared in good to excellent yields. The Sn-β zeolite catalyst also exhibited excellent shape selectivity on the cyclization of meta-substituted 2-aryloxyacetaldehyde acetals, and 6-substituted isomers were preferably formed up to 97% regio-selectivity. Moreover, Sn-β zeolite could be easily recovered and reused without any noticeable activity loss.
- Sun, Nan,Huang, Peng,Wang, Yifan,Mo, Weimin,Hu, Baoxiang,Shen, Zhenlu,Hu, Xinquan
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supporting information
p. 4835 - 4841
(2015/07/27)
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- Thiosemicarbazones as Aedes aegypti larvicidal
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Abstract A set of aryl- and phenoxymethyl-(thio)semicarbazones were synthetized, characterized and biologically evaluated against the larvae of Aedes aegypti (A. egypti), the vector responsible for diseases like Dengue and Yellow Fever. (Q)SAR studies were useful for predicting the activities of the compounds not included to create the QSAR model as well as to predict the features of a new compound with improved activity. Docking studies corroborated experimental evidence of AeSCP-2 as a potential target able to explain the larvicidal properties of its compounds. The trend observed between the in silico Docking scores and the in vitro pLC50 (equals -log LC50, at molar concentration) data indicated that the highest larvicidal compounds, or the compounds with the highest values for pLC50, are usually those with the higher docking scores (i.e., greater in silico affinity for the AeSCP-2 target). Determination of cytotoxicity for these compounds in mammal cells demonstrated that the top larvicide compounds are non-toxic.
- Da Silva, Jo?o Bosco P.,Navarro, Daniela Maria Do A.F.,Da Silva, Aluizio G.,Santos, Geanne K.N.,Dutra, Kamilla A.,Moreira, Diogo Rodrigo,Ramos, Mozart N.,Espíndola, José Wanderlan P.,De Oliveira, Ana Daura T.,Brondani, Dalci José,Leite, Ana Cristina L.,Hernandes, Marcelo Zaldini,Pereira, Valéria R.A.,Da Rocha, Lucas F.,De Castro, Maria Carolina A.B.,De Oliveira, Beatriz C.,Lan, Que,Merz, Kenneth M.
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p. 162 - 175
(2015/06/22)
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- MEDICAMENTS
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A compound of formula (I) is described: wherein R1 and R2 are as defined in the text and wherein the compounds are intended for use in treating medical conditions characterized by an imbalance in dopamine receptor activity.
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Page/Page column 97
(2009/06/27)
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- 4-pyridyl substituted-1,3-dioxane compounds
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The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A1 is alkylene, R1 is a variety of substituents defined hereinafter, and R2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
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- TiCl4 Induced Opening of Chiral Acetals: a route to β-adrenergic blocking agents
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Aryloxy and alkyloxypropanolamines 7a-c are obtained in 45 to 70 percent yields and with asymmetric induction, using TiCl4 induced nucleophilic addition of cyanotrimethylsilane onto chiral acetals derived from racemic 2,4-pentanediol.Therefore, optically pure 2,4-pentanediol will provide, after a purification, optically pure 7a-c.
- Solladie-Cavallo, A.,Suffert, J.,Gordon, M.
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p. 2955 - 2958
(2007/10/02)
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- Bronchodilator and Antiulcer Phenoxypyrimidinones
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Series of 5-phenoxy-2(1H)-pyrimidinones, 5-phenoxy-4(3H)-pyrimidinones, and related compounds were prepared in a follow-up of a lead prepared as a potential cyclic nucleotide regulating agent.Compounds were evaluated for bronchodilator activity in histamine-challenged guinea pigs and for antiulcer activity in a cold-restraint, stressed rat ulcer model.Bronchodilator activity comparable to, or greater than, that of theophylline was found in both the 2(1H)- and 4(3H)-pyrimidinone series and was most prominent in analogues containing either an electron-withdrawing or -donating substituent in the para position of the phenoxy ring.Significant antiulcer activity was observed only in the 2(1H)-pyrimidinone series among three closely related analogues.One of these, 5-(m-methylphenoxy)-2(1H)-pyrimidinone (3), exhibited more potent antiulcer effects than the clinically useful antiulcer agent carbenoxolone, without demonstrating bronchodilator activity.
- Lipinski, C. A.,Stam, J. G.,Pereira, J. N.,Ackerman, N. R.,Hess, H.-J.
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p. 1026 - 1031
(2007/10/02)
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