Methoxylated (E)-arylalkenes (1a–1k) were prepared in two steps by an improved Grignard reaction comprising the reverse addition of alkylmagnesium bromide to benzaldehydes (2a–2k) in anhydrous ether and toluene into arylalkanols (3a–3k) in high yield, followed by dehydration with silica gel under microwave irradiation for 3–12 min, depending upon the substituents attached to the aromatic ring to afford hypolipidemic active α-asarone (1a) and related methoxylated (E)-arylalkenes (1b–1k).
通过改进的Grignard反应,分两步制备了甲氧基化(E)-芳基烯烃(1a-1k)。该反应包括在无
水乙醚和
甲苯中反向加成烷基
镁溴化物至
苯甲醛(2a-2k),高产率地转化为芳基醇(3a-3k),随后在微波辐射下,根据芳香环上取代基的不同,利用
硅胶进行脱
水处理3-12分钟,得到具有降脂活性的α-细辛素(1a)及相关甲氧基化(E)-芳基烯烃(1b-1k)。