发明名称 METABOLITES AND OXIMES WITH VASODILATOR AND HYPOTENSIVE ACTIVITY
摘要 Semi-synthetic oximes derived from metabolites extracted from medicinal plants, Senecio nutans and Xenophyllum poposum, the method of preparation thereof and their use as agents with vasodilator and hypotensive effects are provided.
申请公布号 US2016130219(A1) 申请公布日期 2016.05.12
申请号 US201514876084 申请日期 2015.10.06
申请人 Universidad de Antofagasta 发明人 Paredes Poblete Adrian Guillermo;Morales Borcosque Glauco Segundo;Cifuentes Jorquera Fredi Eduardo
分类号 C07C249/08;C07C251/48;C07D307/79;C07C45/79;C07C249/14 主分类号 C07C249/08
代理机构 代理人
主权项 1. A method of preparing semi-synthetic oximes, comprising: a) applying an extract of S. nutans and/or X. poposum plants to column chromatography and thin layer chromatography, to obtain a metabolite of formula: wherein R corresponds to H, OH or methyl; R′ and R″ corresponds to H, methyl, propyl, propylene, 3-methylbutyl-2-ene, or R′ y R″ together form a system derived from dihydrobenzofuran, b) heating under reflux between 100 mg to 400 mg of starting metabolite with a mixture of from 30 to 250 mg of hydroxylamine hydrochloride dissolved in 5 mL of ethanol and from 150-400 μL of pyridine at 40° C.-60° C. for 18-38 hours; c) separating the organic phase from the reaction mixture by liquid-liquid extraction using an organic solvent such as dichloromethane, chloroform, ethyl acetate or ethyl ether; d) concentrating the organic phase on a rotary evaporator; e) purifying the oxime by silica gel column chromatography, wherein each column progress is monitored by thin layer chromatography.
地址 Antofagasta CL