5300-22-1Relevant articles and documents
Method for preparing [alpha]-(methylaminoethyl)benzyl alcohol by adopting micro-flow field reaction technology
-
Paragraph 0016-0051, (2021/01/15)
The invention discloses a method for preparing [alpha](methylaminoethyl) benzyl alcohol by using a micro-flow field reaction technology, which comprises the following steps: by using styrene and ethylamine as raw materials and 1, 3-dibromo-5, 5-dimethylhydantoin (DDH) as a catalyst, preparing by using a micro-channel modular reaction device, wherein the micro-channel modular reaction device comprises a micro-structure mixer, a micro-structure reactor 1 and a micro-structure reactor 2 which are sequentially connected through a pipeline, and the method comprises the following steps: (1) respectively dissolving styrene and 1, 3-dibromo 5, 5-dimethyl hydantoin in a solvent, mixing through the micro-structure mixer, and injecting into the micro-structure reactor 1 for reaction; and (2) dissolving ethylamine in a solvent, injecting ethylamine and the reaction solution obtained in the step (1) into a microstructure mixer 2 together, mixing, introducing into a microstructure reactor 2, reacting, and collecting the product after the reaction to obtain [alpha]-(methylaminoethyl)benzyl alcohol. The method has the advantages of high catalytic efficiency, mild and simple reaction conditions, high product yield, convenience in operation and the like.
Optimization of immobilization conditions of Mucor miehei lipase onto Florisil via polysuccinimide spacer arm using response surface methodology and application of immobilized lipase in asymmetric acylation of 2-amino-1-phenylethanols
Yildirim, Deniz,Tuekel, S. Seyhan,Alptekin, Oezlem,Alagoez, Dilek
, p. 91 - 103 (2014/01/17)
In this study, the immobilization of Mucor miehei lipase onto Florisil support via polysuccinimide spacer arm was scrutinized by using a 3-factor and 3-level Box-Behnken design. The independent parameters were immobilization pH, immobilization time and initial lipase concentration and the response was the specific activity of immobilized lipase. A quadratic equation was used to explain the relationship between the response and independent parameters. After analysis of variance test, coefficient of determination and adjusted coefficient of determination values were estimated as 0.98 and 0.94, respectively. The optimal immobilization pH, immobilization time and initial lipase concentration were determined as 6.0, 7 h and 1.1 mg mL-1, respectively, after desirability analysis. The specific activity values for three individual experiments were observed as 25.88 ± 0.73, 26.06 ± 0.47 and 25.96 ± 0.52 U mg protein-1 under the optimized conditions. The hydrolytic activities of free and immobilized lipase preparations were characterized using p-nitrophenyl palmitate as substrate. The esterification activity of immobilized lipase preparation was evaluated by asymmetric acylation of 2-(methylamino)-1-phenylethanol, 2-(ethylamino)-1- phenylethanol, 2-(butylamino)-1-phenylethanol, and 2-(hexylamino)-1- phenylethanol with vinyl acetate. The acylation protocol was optimized in terms of the effects of initial water amount, reaction temperature, molar ratio of amino alcohol to vinyl acetate, biocatalyst loading, organic medium and kind of lipases used. The developed protocol provided a facile methodology for the preparation of enantiopure 2-amino-1-phenylethanols which may be used as potential new β-adrenergic receptor antagonists.
ANTIFUNGAL COMPOUNDS
-
Page/Page column 37, (2012/10/08)
The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.