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青蒿素降解产物双酮(1)与氢氧化钡反应生成不饱和酮酸(5)。(5)的构型已由X射线单晶衍射测定。(5)与Wittig试剂反应,得到双烯(7a)。以Raney Ni作催化剂氢化双烯(7a)生成二氢青蒿酸(9a)和它的异构体(10a)以及少量全氢化产品(11a)。用四氧化锇和N-甲基吗啉-N-氧化物处理氢化产物,分离得到(9a)的衍生物羟基内酯(12)。
The artemisinin biodegradation product diketone (1) reacts with barium hydroxide to form unsaturated keto acid (5). The configuration of (5) has been determined by X-ray single crystal diffraction. (5) is reacted with Wittig reagent to give the diolefin (7a). Hydrogenation of the diolefins (7a) with Raney Ni as a catalyst yields dihydroartemisinic acid (9a) and its isomers (10a) as well as small quantities of the fully hydrogenated product (11a). The hydrogenated product is treated with osmium tetroxide and N-methylmorpholine-N-oxide and the derivative hydroxylactone (12) of (9a) is isolated.