Epoxidation of Primary and Secondary Alkenylammonium Salts with Dimethyldioxirane, Methyl(trifluoromethyl)dioxirane, and m-Chloroperbenzoic Acid. A General Synthetic Route to Epoxyalkylamines
摘要:
Selective syn-epoxidation of C=C double bonds in primary and secondary alkenylammonium arenesulfonate salts 3H(+), to give the corresponding epoxyalkylammonium salts 4H(+), has been achieved by reaction with electrophilic O-transfer reagents such as m-CPBA, methyl(trifluoromethyl)dioxirane (TFDO), and dimethyldioxirane (DMDO). Epoxyalkylamines 4 are easily obtained in high yields from the corresponding epoxyalkylammonium salts 4H(+) by simple deprotonation with sodium carbonate. The ammonium group deactivates the C=C double bond, and hence the epoxidation rate is slower than in the case of simple olefins. II-Bonding interaction between the ammonium group and the O-transfer reagent(m-CPBA and DMDO) in the transition state is claimed to account for the rate enhancement and diastereoselectivity observed when the necessary conformational requirements are established. The allylic ammonium group is shown to be very efficient in directing the epoxidation with m-CPBA and DMDO on the syn-diastereoface.
CATALYST FOR SYNTHESIZING ETHYLENIMINE AS WELL AS PREPARATION METHOD AND APPLICATION THEREOF
申请人:XI'AN MODERN CHEMISTRY RESEARCH INSTITUTE
公开号:US20160318863A1
公开(公告)日:2016-11-03
The present invention relates to a catalyst for synthesizing ethylenimine as well as a preparation method and application thereof. The related catalyst comprises a carrier and metal ions loaded on the carrier; the carrier is a composite oxide comprising titanium, silicon and phosphorus elements; the metal ions are magnesium ions, iron ions and cesium ions; the molar ratio of the magnesium ions to the iron ions to the cesium ions is (1-10):1:0.1; the mass of all metal ions is 0.5-10 percent of that of the carrier. In the related preparation method, a catalyst precursor is roasted at the temperature of 350-650° C., so that the catalyst is obtained; the catalyst precursor is the mixture of the carrier, soluble salt of magnesium, soluble salt of iron and soluble salt of cesium. The present invention also provides the application of the catalyst to synthesis of the ethylenimine by using amino alcohol as the raw material. Compared with a common catalyst which has the requirement on the temperature of over 400° C., the catalyst of the present invention obviously reduces the reaction temperature. The prepared catalyst can catalyze the intramolecular dehydration reaction of the amino alcohol and has relatively excellent selectivity.
Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring
作者:Chetan M. Bhalgat、Pooja V. Darda、Kailash G. Bothara、Shashikant V. Bhandari、Jotsna Gandhi、B. Ramesh
DOI:10.1016/j.ejmech.2014.02.048
日期:2014.4
analysis, IR, 1H NMR, 13C NMR and mass spectral data and tested for electrocardiographic, antiarrhythmic and antihypertensive activities. Compound 11 was found to be most potent in this series. The pharmacological results suggested that, the antiarrhythmic effects of these compounds were related to their Ca++ ion channel antagonistic properties, which are believed to be due to the presence of 5-benzilid
在本研究中,合成了包含5-亚苄基-2-(苯基亚氨基)-噻唑烷丁-4-酮部分的十四种衍生物。通过元素分析,IR,1 H NMR,13 C NMR和质谱数据确定合成的化合物的结构,并测试其心电图,抗心律不齐和降压活性。发现化合物11在该系列中最有效。药理结果表明,这些化合物的抗心律失常作用与其Ca ++有关离子通道的拮抗特性,据信归因于5-苯甲啶-2-(苯基亚氨基)-噻唑烷丁-4-酮部分的存在。较小体积的脂族和杂环叔胺的存在会增强β-受体侧链的降压作用。