Selective hydroaminomethylation of olefins using simple and efficient Rh-phosphinite complex catalyst
作者:Shoeb R. Khan、Bhalchandra M. Bhanage
DOI:10.1002/aoc.3046
日期:2013.12
Hydroaminomethylation of various olefins with primary and secondary amines was carried out using a simple and efficient rhodium–phosphinite complexcatalyst. The influence of various reaction parameters including the effects of temperature, pressure, catalyst loading, time and solvents has been investigated. The present protocol is general with wider substrate applicability for the synthesis of an
Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain.
Rhodium complex encapsulated functionalized hexagonal mesoporous silica for heterogeneous hydroaminomethylation
作者:N. Sudheesh、Ram S. Shukla
DOI:10.1016/j.apcata.2012.12.021
日期:2013.2
HRh(CO)(PPh3)(3) complex was encapsulated into the pores of amino functionalized hexagonal mesoporous silica. The catalyst was characterized by physico-chemical techniques like P-XRD, P-31-CPMAS NMR, FT-IR, SEM, ICP and N-2 adsorption analysis. The catalyst was active for hydroaminomethylation and a variety of alkenes and amines were used as reactants for hydroaminomethylation. The catalyst afforded to achieve 100% conversion with high (>95%) selectivity to corresponding amines. Parametric variations were performed by taking 1-hexene and morpholine as representative reactants for the study of catalyst amount, temperature, pressure and 1-hexene:morpholine ratio. Significant amounts of aldehydes and enamines were observed during the course of the reaction indicating that there could be two possible rate determining steps. The catalyst was effectively recycled up to five times without much loss in its activity and selectivity. (C) 2012 Elsevier B.V. All rights reserved.
PSYCHOTROPIC AGENTS AND USES THEREOF
申请人:LB PHARMACEUTICALS INC.
公开号:US20180155282A1
公开(公告)日:2018-06-07
Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain, either individually or in combination with other CNS active agents.
Rhodium exchanged ETS-10 and ETS-4: Efficient heterogeneous catalyst for hydroaminomethylation
作者:N. Sudheesh、Ram S. Shukla
DOI:10.1016/j.apcata.2014.01.002
日期:2014.3
Rhodium exchanged titanosilicates (ETS-10 and ETS-4) were synthesized and found to be efficient and stable catalysts for hydroaminomethylation reaction. The catalyst was highly active and selective towards amine product within lower reaction time of 4 h. 1-Hexene and pyrrolidine were taken as representative substrates for parametric variations using Rh-ETS-10. The increase in pyrrolidine ratio gave some significant information showing a decrease in conversion with increased selectivity. The reason may be the competition between pyrrolidine and 1-hexene for coordination sites in rhodium and which prevents the beta-hydride elimination. The ratios of H-2 and CO have influenced hydroaminomethylation and the best performance was in the CO: H-2 ratio of 1:4 under the studied conditions. The initial rate of formation of amine was double than that of isomerization of 1-hexene. The Rh cluster like complex was formed on treating the catalyst with syn gas. A homogenous-heterogeneous dual nature of Rh was found during hydroaminomethylation. The catalyst was effectively recycled for three times without much loss in its activity and selectivity. (C) 2014 Elsevier B.V. All rights reserved.