Catalyst-Free Transamidation of Aromatic Amines with Formamide Derivatives and Tertiary Amides with Aliphatic Amines
作者:Jiawen Yin、Jingyu Zhang、Changqun Cai、Guo-Jun Deng、Hang Gong
DOI:10.1021/acs.orglett.8b03542
日期:2019.1.18
A simple catalyst- and promoter-free protocol has been developed for the transamidation of weakly nucleophilic aromatic amines with formamide derivatives and low-reactivity tertiary amides with aliphatic amines. This strategy is advantageous because no catalyst or promoters are needed, no additives are required, separation and purification is easy, and the reaction is scalable. Significantly, this
Anticancer potential of aminomethylidene-diazinanes I. Synthesis of arylaminomethylidene of diazinetriones and its cytotoxic effects tested in glioblastoma cells
作者:Nichole A. Pianovich、Mathew Dean、Adam Lassak、Krzysztof Reiss、Branko S. Jursic
DOI:10.1016/j.bmc.2017.08.020
日期:2017.10
Diazinane and aryl moieties with vinylamine linkers were synthesized to investigate the importance of their structural variations as potential anti-glioblastoma agents. Structural variations incorporated on to the diazinane moiety included oxa and thio derivatives, each with a variety of nitrogen-bound substituents. The size and shape of the aromatic moiety was varied, with the final variation introducing two carbonyl groups, yielding a substituted anthraquinone. Readily available diazinanes and aryl amines were used as an advantageous foundation. Several parameters were calculated whilst engineering these compounds, including: Clog P, molecular polarizability, polar surface area, minimal molecular projected area, and pK(a). In addition, a simple and efficient procedure was developed to synthesize these compounds. It was demonstrated that a vinylamine with 1,3-diazinane-2,4,6-trione and 1-anthraquinone moiety is the most promising drug candidate causing almost 70% of LN229 tumor cell death at 1 mu g/ml. In addition, its molecular polarizability, polar surface area and minimal molecular projected area indicate a possible potential of this molecule for crossing BBB. (C) 2017 Published by Elsevier Ltd.
[EN] BENZOYLUREA COMPOUND AND USE THEREOF<br/>[FR] COMPOSE BENZOYLUREE ET SON UTILISATION
申请人:SUMITOMO CHEMICAL CO
公开号:WO2007066496A1
公开(公告)日:2007-06-14
[EN] The present invention relates to a benzoylurea compound represented by the formula (1): wherein R2 represents a lower alkylene group etc., and A represents a group represented by OR3, S(O) nR4 or NR5R6, or a salt thereof, and use of the same for controlling pests. [FR] La présente invention concerne un composé benzoylurée représenté par la formule (1) : dans laquelle R2 représente un groupe alkylène inférieur, etc. et A représente un groupe représenté par OR3, S(O)nR4 ou NR5R6, ou un sel de celui-ci, et son utilisation pour lutter contre les parasites.