Synthesis of angiotensin II receptor blockers by means of a catalytic system for C-H activation.
A highly efficient catalytic system for C-H activation has been worked out that involves inexpensive RuCl(3)·xH(2)O and a specific amount of PPh(3). This procedure has been successfully applied to a practical synthesis of angiotensin II receptor blockers (ARBs). The residual ruthenium that existed in the reaction mixture was thoroughly removed by treatment with properly selected metal scavengers. The new process permits ready access to the important class of drugs in a highly atom-economical and sustainable manner.
Process Research & Development Laboratory, API Corporation 1-1, Shiroishi, Kurosaki, Yahatanishi-ku, Kitakyushu, Fukuoka 806-0004, Japan. seki.masahiko@mm.api-corp.co.jp
Masahiko
M
Seki
Masaki
M
Nagahama
D057911:Angiotensin Receptor Antagonists / Q000138:chemical synthesis*; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001713:Biphenyl Compounds / Q000737:chemistry; D002384:Catalysis; D002614:Chelating Agents / Q000737:chemistry; D006801:Humans; D019808:Losartan / Q000138:chemical synthesis*; D009682:Magnetic Resonance Spectroscopy; D012428:Ruthenium; D013777:Tetrazoles / Q000138:chemical synthesis*; D013778:Tetrazolium Salts / Q000138:chemical synthesis*; D014633:Valine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D000068756:Valsartan
D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D001713:Biphenyl Compounds; D002614:Chelating Agents; D019808:Losartan; D012428:Ruthenium; D013777:Tetrazoles; D013778:Tetrazolium Salts; D014633:Valine; D000068756:Valsartan; C003110:phenyltetrazolium; C010574:biphenyl