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以查尔酮和对甲苯磺酰甲基异氰(TosMIC)为原料,使用改进的Van Leusen合成法,在DMSO溶剂中,通过金属钠和DMSO反应生成的NaCH2SOCH3为催化剂,合成了12个片螺素结构简化物,并用IR和1HNMR对所合成的化合物结构进行了表征。结果表明,在反应温度25~50℃,反应时间30~120 min的条件下,该法的合成产率可达63%~82%。该法避免了传统的Van Leusen方法中使用NaH作为催化剂、乙醚作为溶剂所带来的价格昂贵和容易着火等问题,便于放大合成和工业化生产。
Using Chalcone and p-toluenesulfonylmethylisocyanurate (TosMIC) as raw materials, a modified Van Leusen method was used to synthesize 12 snails by using NaCH 2 SOCH 3 produced by the reaction between sodium metal and DMSO in DMSO. The structures of the compounds were characterized by IR and 1HNMR. The results showed that under the conditions of reaction temperature of 25 ~ 50 ℃ and reaction time of 30 ~ 120 min, the synthetic yield of this method can reach 63% -82%. The method avoids the traditional Van Leusen method using NaH as a catalyst, ether as a solvent brought about expensive and easy to fire and other issues, easy to enlarge the synthesis and industrial production.