新型白藜芦醇吡唑衍生物的合成工艺研究

Study on Synthesis of Novel Pyrazole Derivative of the Resveratrol

在氢氧化钠存在下,白藜芦醇衍生物(E)-2,4-二甲氧基-6-(4-甲氧基苯乙烯基)苯甲醛与丙酮经Claisen-Schmidt缩合反应合成化合物B,收率为77.68%。化合物B和对甲苯磺酰肼在氢氧化钠为缚酸剂,(n-Bu)4NBr为相转移催化剂且用量为化合物B的2 equiv的条件下,于80℃反应12 h,得到产物(E)-3-(2-(4-甲氧基苯乙烯基)-4,6-二甲氧基苯基)-5-甲基-1H-吡唑,收率为59.13%。该方法具有合成成本低、工艺操作简便和经济性好等优点。

First, compound B was prepared by the Claisen-Schmidt condensation between （E）-2, 4-dimethyl-6- （4-methoxystyryl） benzaldehyde and acetone in the presence of NaOH in 77.65 % yield. Compound C was obtained by the cyclization reaction between compound B and p-Toluenesulfonohydrazide at 80℃ for 12 h, using sodium hydroxide as base, （n-Bu）4NBr as phase transfer catalyst and the amount of （n-Bu）4NBr was 2 equiv of compound B. The yield of compound C was 59.13%. The synthetic method had the advantages of low cost, easy to operate and good economy.