【摘要】 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。更多还原

【Abstract】 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.更多还原