2,2-二甲基苯并吡喃类衍生物的合成

目的 设计合成一系列苯并吡喃类衍生物。方法 以2-甲基-丁-3-炔-2-醇为起始原料，经氯代、Williamson 成醚、环合、Aldol 缩合4步反应得到目标化合物。结果与结论 合成了16个未见文献报道的新化合物，其结构经¹H-NMR 和 MS 谱确定。所有目标化合物的抗肿瘤活性测试正在进行中。

Synthesis of 2,2-dimethyl benzopyran derivatives

2,2-dimethyl benzopyran derivatives, derived from natural products and with a lot of bioactivities including antitumor, smooth muscle relaxation etc., is a good lead compound of antitumor, because of its excellent bioactivities, relative simple molecular structure. So sixteen novel target compounds (Compd.1a-1p) were designed and synthesized. Treatment of 2-methylbut-3-yn-2-ol with concentrated hydrochloric acid gave 3-chloro-3-methylbut-1-yne, which was reacted with 4-hydroxybenzaldehyde and followed by cyclization to afford 2,2-dimethyl-2H-chromene-6-carbaldehyde. The target compounds were obtained by the reaction of 2,2-dimethyl-2H-chromene-6-carbaldehyde with the corresponding substituted ketone, and their structures were confirmed by ¹H-NMR and ESI-MS.