呫吨类抗胆碱能化合物的合成研究

Synthesis of Anticholinergic 9-Hydroxy-9-xanthenecarboxylates

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30kg/cm2,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.

A series of new 9-hydroxy-9-xanthenecarboxylates were designed and synthesized. In the synthesis of the tricyclic group, the preparation of disubstituted xanthene derivatives was studied. In the synthesis of the amino alcohol, the 10% Pd/C was used as the catalysts, the pressure was dropped to 30 kg/cm^2, 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.