呫吨类抗胆碱能化合物的合成研究有机化学.pdfVIP

2009 年第 29 卷 有 机 化 学 Vol. 29, 2009 第 6 期, 942～947 Chinese Journal of Organic Chemistry No. 6, 942～947 ·研究论文· 呫吨类抗胆碱能化合物的合成研究 弓亚玲 陆模文 孔 博 胡文祥* (首都师范大学化学系 北京 100048) 摘要 呫吨羟基羧酸酯类化合物是一类新型高效的抗胆碱、抗梭曼化合物, 比以往的抗胆碱药物效价有较大幅度的提 高，设计合成了一系列新的 9-羟基-9-呫吨羧酸酯类抗胆碱化合物. 在合成环状基团的过程中, 探索了取代呫吨环中间 2 体的合成路线; 在氨基醇的合成过程中, 采用 10%的Pd/C 作催化剂, 并将 H2 的压力下降到30 kg/cm , 产率提高到 90%, 优化了催化氢化的反应条件; 在目标化合物的合成过程中, 改进了产物的纯化和后处理方法, 简化了操作步骤. 关键词 呫吨; 羟基羧酸酯; 9-羟基-9-呫吨羧酸酯; 氨基醇 Synthesis of Anticholinergic 9-Hydroxy-9-xanthenecarboxylates Gong, Yaling Lu, Mowen Kong, Bo Hu, Wenxiang* (Department of Chemistry, Capital Normal University, Beijing 100048) Abstract A series of new 9-hydroxy-9-xanthenecarboxylates were designed and synthesized. In the syn- thesis of the tricyclic group, the preparation of disubstituted xanthene derivatives was studied. In the synthe- 2 sis of the amino alcohol, the 10% Pd/C was used as the catalysts, the pressure was dropped to 30 kg/cm , the conditions for hydrogenation reactions were optimized, and the yield of the reaction was increased. For the synthesis of target compounds, the post-treatment and purification methods were improved and at the same time, the procedures were simplified. Keywords xanthene; hydroxycarboxylate; methyl 9-hydroxyl-9-xanthenecarboxylate; amino alcohol 抗胆碱药的应用和研究具有悠久的历史,