首页|枸橼酸坦度螺酮的合成改进

枸橼酸坦度螺酮的合成改进

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以2-氯嘧啶为起始原料,经N-烃基化、季铵化、亲核取代、成盐等反应合成了枸橼酸坦度螺酮.对影响收率的缚酸剂、反应温度、溶剂、催化剂等因素进行了工艺优化.优化后总收率65.2%,产品纯度99.9%.枸橼酸坦度螺酮及中间体的结构经1HNMR和ESI-MS确证.其工艺操作简单,原料价廉易得,具有工业化应用前景.
Improvement on the Synthesis of Tandospirone Citrate
Tandospirone citrate was synthesized from 2-chloropyrimidine via a processes including N-hydrocarbylation,quaternization,nucleophilic and salify with a total yield of 65.2%and a chromatographic purity of 99.9%.The affecting factors including the acid-binding regent,the reaction temperature,solvent and the catalyst were investigated.The structures of the product and intermediates were characterized by 1H NMR and ESI-MS.The preparation process was simple in operation,low in raw material cost,and suitable for industrial production.

tandospirone citrateimprovementN-hydrocarbylationnucleophilic

徐大伟、王志轩、程青芳

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连云港康乐药业有限公司,江苏连云港 222008

江苏海洋大学药学院,江苏连云港 222005

枸橼酸坦度螺酮 改进 N-烃基化 亲核取代

2024

精细化工中间体
湖南化工研究院

精细化工中间体

CSTPCD
影响因子:0.236
ISSN:1009-9212
年,卷(期):2024.54(1)
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