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安立生坦的合成研究

张青扬, 吕久安, 胡海宇

张青扬, 吕久安, 胡海宇. 安立生坦的合成研究[J]. 中国药科大学学报, 2017, 48(3): 293-296. DOI: 10.11665/j.issn.1000-5048.20170307
引用本文: 张青扬, 吕久安, 胡海宇. 安立生坦的合成研究[J]. 中国药科大学学报, 2017, 48(3): 293-296. DOI: 10.11665/j.issn.1000-5048.20170307
ZHANG Qingyang, LYU Jiuan, HU Haiyu. Synthesis of(+)-ambrisentan[J]. Journal of China Pharmaceutical University, 2017, 48(3): 293-296. DOI: 10.11665/j.issn.1000-5048.20170307
Citation: ZHANG Qingyang, LYU Jiuan, HU Haiyu. Synthesis of(+)-ambrisentan[J]. Journal of China Pharmaceutical University, 2017, 48(3): 293-296. DOI: 10.11665/j.issn.1000-5048.20170307

安立生坦的合成研究

Synthesis of(+)-ambrisentan

  • 摘要: 以二苯甲酮为原料,经5步反应得到安立生坦,并优化了拆分和取代步骤。在拆分步骤中采用化学性质稳定且便于检测的 L-苯甘氨酰胺作为拆分试剂,获得具有较高光学纯度的中间体。在取代反应中采用安全性较高的氢氧化钠作为强碱,适合工业生产。该工艺反应条件温和,操作简便,总收率达到31.0%,具有良好的应用前景。
    Abstract: A five-step synthetic method of ambrisentan starting from benzophenone was developed. The reaction methods of resolution and substitution were optimized. A stable, facilitating method of detection and efficient resolution reagent, L-phenylglycinamide, was used and helped to obtain highly optical pure intermediates. In the substitution reaction, NaOH was chosen as the base, which is safe and suitable for the industry. This method was mild, easily operated with a total yield up to 31. 0%, and may have a good application prospect.
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出版历程
  • 刊出日期:  2017-06-24

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