• Corpus ID: 20991783

Improved Synthesis Process of Ambrisentan and Darusentan

  title={Improved Synthesis Process of Ambrisentan and Darusentan},
  author={J. Li and Ling Tian},
  journal={Chemical engineering transactions},
  • J. LiL. Tian
  • Published 20 December 2015
  • Chemistry
  • Chemical engineering transactions
2-hydroxy-3-phenoxy-3, 3-diphenylpropinate (5) was prepared from benzophenone via Darzens, methanolysis and hydrolysis reaction. The compound (5) was salified with (S)-dehydroabietylamine (7) and diasterotropic resolution was carried out to provide the key intermediate (S)-2-hydroxy-3-methoxy-3, 3-diphenylpropionic acid (6). Compound (6) was condensed with 2-methylsulfonyl-4, 6-dimethylpyrimidine and 2-methoxysulfonyl4, 6-dimethylpyrimidine to afford ambrisentan (1) and darusentan (7… 

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