Benzimidazole-carboxamides as potent and bioavailable stearoyl-CoA desaturase (SCD1) inhibitors from ligand-based virtual screening and chemical optimization
摘要:
The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was selected for further pharmacological profiling based on favorable in vitro data. After oral administration to male ZDF rats, this compound significantly decreased the serum fatty acid desaturation index, thus providing conclusive evidence for SCD1 inhibition in vivo by SAR224. (C) 2013 Elsevier Ltd. All rights reserved.
[EN] A METHOD OF ACETALIZING AN ALDEHYDE<br/>[FR] PROCÉDÉ D'ACÉTALISATION D'UN ALDÉHYDE
申请人:AGENCY SCIENCE TECH & RES
公开号:WO2013137830A1
公开(公告)日:2013-09-19
A method of acetalizing an aldehyde comprising reacting said aldehyde with an alcohol in the presence of a polymeric catalyst to form an acetal wherein the polymeric catalyst is a mesoporous poly-melamine-formaldehyde polymer.
一种使醛发生缩醛化的方法,包括将所述醛与醇在多孔聚三聚氰胺-甲醛聚合物的催化下反应,形成缩醛。
METHOD FOR PRODUCING CARBONATE DERIVATIVE
申请人:NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY
公开号:US20210403409A1
公开(公告)日:2021-12-30
The objective of the present invention is to provide a method for producing a polycarbonate safely and efficiently even without using a base. The method for producing a carbonate derivative according to the present invention is characterized in comprising the step of irradiating a high energy light to a composition comprising the halogenated methane and the hydroxy group-containing compound in the presence of oxygen, wherein a molar ratio of a total usage amount of the hydroxy group-containing compound to 1 mole of the halogenated methane is 0.05 or more.
Reaction of 2-aryl-1,3-dioxane with arenes in the presence of a catalytic amount of trifluoromethanesulfonic acid gave the corresponding diarylmethanes in good to excellent yields. The acid-catalyzed Friedel-Crafts benzylation of arenes could altenatively be carried out using arenecarbaldehyde and 1,3-propanediol. The reaction was assumed to proceed through a redox process involving hydride shift from the cyclic acetal moiety to the benzylic carbon. The hydride shift was confirmed by the reaction with 5-ethyl-2-phenyl-4,4,6,6-tetradeuterio-1,3-dioxane, wherein more than 90% deuterium was incorporated into the benzylic carbon of the diphenylmethane. Diphenylmethyl ether Ph(2)CHOCH(2)CH(2)CH(2)OH also reacted with benzene to afford diphenylmethane under the same reaction conditions, suggesting that the ether should be the plausible intermediate that underwent the hydride shift.
METHOD FOR PRODUCING POLYCARBONATE
申请人:NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY
公开号:US20210388159A1
公开(公告)日:2021-12-16
The objective of the present invention is to provide a method for producing a polycarbonate safely and efficiently. A method for producing a polycarbonate is characterized in comprising the step of irradiating a light to a composition comprising a C
1-4
halogenated hydrocarbon, the specific diol compound and the specific base in the presence of oxygen.
Mesoporous poly-melamine-formaldehyde (mPMF) – a highly efficient catalyst for chemoselective acetalization of aldehydes
作者:Mei Xuan Tan、Liuqun Gu、Nannan Li、Jackie Y. Ying、Yugen Zhang
DOI:10.1039/c3gc40297e
日期:——
A mesoporous poly-melamine-formaldehyde polymer with a high surface area, good porosity and a high density of amine and triazine functional groups was investigated as a highly efficient hydrogen-bonding catalyst. This porousorganicpolymer was found to be highly effective in catalyzing chemoselective acetalization of aldehydes, without the consumption of any dehydrating agents. The turnover frequency