3-(3-氯-1,2,5-噻二唑-4-基)吡啶的合成工艺改进

Improved synthesis of 3-(3-chloro-1,2,5-thiadiazol-4-yl)pyridine

以3-吡啶甲醛为原料,与氰化钠、一氯化硫反应合成选择性M1受体激动剂占诺美林的关键中间体3-(3-氯-1,2,5-噻二唑-4-基)吡啶,目标化合物的结构经1H-NMR谱确证。改进后的工艺操作简单,反应条件温和,收率由文献报道的40%提高到52%,更适合工业化生产。

3-（3-Chloro-1,2, 5-thiadiazol-4-yl）pyridine, which is a key intermediate of selective M1 receptor agonist xanomeline, was synthesized from 3-pyridine carboxaldehyde, sodium cyanide, and sulfur chloride. This procedure has advantage of convenient operations and mild reaction conditions. The yield is improved from 40 % to 52 % and the process is easy to be popularized in industry.