Search

Aziridines derived from bioactive molecules may have unique pharmacological activities, making them useful in pharmacology (e.g. mitomycin C). Furthermore, the substitution of the epoxide moiety in epothilone B with aziridine, an analog of epoxides, yielded a pronounced enhancement in its anticancer efficacy. Thus, there is interest in developing novel synthetic technologies to produce aziridines from bioactive molecules. However, known methods usually require metal catalysts, stoichiometric oxidants and/or pre-functionalized amination reagents, causing difficulty in application. A practical approach without a metal catalyst and extra-oxidant for the aziridination of bioactive molecules is in demand, yet challenging. Herein, we report an electro-oxidative flow protocol that accomplishes an oxidant-free aziridination of natural products. This process is achieved by an oxidative sulfonamide/alkene cross-coupling, in which sulfonamide and alkene undergo simultaneous oxidation or alkene is oxidized preferentially. Further anticancer treatments in cell lines have demonstrated the pharmacological activities of these aziridines, supporting the potential of this method for drug discovery. [ABSTRACT FROM AUTHOR]

为探究菜籽油中是否存在内源性香兰素,对不同产地、加工工段、炒制温度的油菜籽及菜籽油中香兰素、甲基香兰素和乙基香兰素进行了检测。结果表明：所有样本中均未检出甲基香兰素和乙基香兰素；不同产地油菜籽中香兰素含量差异较大，含量范围为123.55～1 669.25 μg/kg；加工过程中，炒制油菜籽中香兰素含量较炒制前大幅增加，且其压榨菜籽饼中的香兰素含量高于压榨菜籽原油中的；随着炒制温度的上升，炒制油菜籽、压榨菜籽原油、压榨菜籽饼中香兰素含量增加，含量范围为189.93～5 080.00 μg/kg。综上，油菜籽中存在内源性香兰素，不能将菜籽油及其调和油中检测出香兰素作为判定添加了外来香兰素的标准。In order to explore the presence of endogenous vanillin in rapeseed oil, vanillin, methyl vanillin and ethyl vanillin in rapeseed and rapeseed oil from different origins, processing sections and roasting temperatures were detected. The results showed that methyl vanillin and ethyl vanillin were not detected in all samples. The content of vanillin in rapeseed from different origins varied greatly, ranging from 123.55 μg/kg to 1 669.25 μg/kg. During processing, the content of vanillin in roasted rapeseed was higher than that before roasting, and the content of vanillin in pressed rapeseed cake was higher than that in the crude pressed rapeseed oil. With the increase of roasting temperature, the content of vanillin in roasted rapeseed, crude pressed rapeseed oil, and pressed rapeseed cake increased, ranging from 189.93 μg/kg to 5 080.00 μg/kg. In summary, there are endogenous vanillin in the rapeseed, and the detection of vanillin in rapeseed oil and its blended oil cannot be used as a criterion to determine the addition of exogenous vanillin.