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以E-1-(2,4,5-三甲氧基苯基)-2-丙烯(α-细辛脑)为原料,酸催化选择性合成脱碳木脂素类化合物a及二氢化茚类化合物b,其结构经核磁﹑质谱和元素分析表征确认.研究了催化剂种类、反应溶剂和温度等条件对两种化合物产率比的影响,45℃时,HCl为催化剂,乙醇为溶剂,化合物a/b的总收率为98%(a:41%,b:57%);30℃时,AlCl3为催化剂,乙醇为溶剂,化合物a的产率可达75%,没有b生成,对a的选择性为100%;45℃时,以BF3Et2O溶液为催化剂,CH2Cl2为溶剂,化合物a的产率为20%,化合物b的产率可达60%.采用MTT法,分别评价了化合物a/b对四种癌细胞(MCF-7,Bel-7402,A549及Hela)的抑制作用,结果表明:化合物a对MCF-7,Hela(IC50值分别为:120.2,117.3μmol L-1),化合物b则对MCF-7,A549(IC50值分别为:66.1,72.4μmol L-1)显示出比相同条件下5-Fu更好的抗癌抑制活性.同时,研究了a/b浓度﹑作用时间对癌细胞抑制率的影响.
The acid catalyzed selective synthesis of decarboxylated lignosin compounds a and indane derivatives with E-1- (2,4,5-trimethoxyphenyl) -2-propene The structure of compound b was confirmed by 1H NMR, MS and elemental analysis. The influences of the type of catalyst, reaction solvent and temperature on the yields of the two compounds were studied. At 45 ℃, HCl was used as catalyst and ethanol as solvent. Compound a / b was 98% (a: 41%, b: 57%). When AlCl3 was used as the catalyst and ethanol was used as the solvent at 30 ℃, the yield of compound a could reach 75% Selectivity was 100%, the yield of compound a was 20% and the yield of compound b was 60% with BF3Et2O solution as catalyst and CH2Cl2 as solvent at 45 ℃ .MTT method was used to evaluate the effects of compound a / b The inhibitory effect of compound a on MCF-7, Hela (IC50 values: 120.2,117.3μmol L-1), compound b (MCF-7, Bel-7402, A549 and Hela) MCF-7, A549 (IC50 values: 66.1, 72.4μmol L-1, respectively) showed better anticancer activity than 5-Fu under the same conditions.Meanwhile, the effect of a / b concentration, Cancer cell inhibition rate.