Synthesis of(+)-ambrisentan

ZHANG Qingyang; LYU Jiuan; HU Haiyu

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

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

Synthesis of(+)-ambrisentan

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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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Synthesis of(+)-ambrisentan

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