精细化工中间体2024,Vol.54Issue(1) :25-29.DOI:10.19342/j.cnki.issn.1009-9212.2024.01.006

枸橼酸坦度螺酮的合成改进

Improvement on the Synthesis of Tandospirone Citrate

徐大伟 王志轩 程青芳
精细化工中间体2024,Vol.54Issue(1) :25-29.DOI:10.19342/j.cnki.issn.1009-9212.2024.01.006

枸橼酸坦度螺酮的合成改进

Improvement on the Synthesis of Tandospirone Citrate

徐大伟 1王志轩 2程青芳2
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作者信息

  • 1. 连云港康乐药业有限公司,江苏连云港 222008
  • 2. 江苏海洋大学药学院,江苏连云港 222005
  • 折叠

摘要

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.

Abstract

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.

关键词

枸橼酸坦度螺酮/改进/N-烃基化/亲核取代

Key words

tandospirone citrate/improvement/N-hydrocarbylation/nucleophilic

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出版年

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
参考文献量11
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