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 RuCl3·xH2O and a specific amount of PPh3. This procedure has been successfully applied to a practical synthesis of angiotensin II receptor blockers (ARBs). The residual ruthenium that existed in the...

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Veröffentlicht in:Journal of organic chemistry 2011-12, Vol.76 (24), p.10198-10206
Hauptverfasser: Seki, Masahiko, Nagahama, Masaki
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Nagahama, Masaki
description A highly efficient catalytic system for C–H activation has been worked out that involves inexpensive RuCl3·xH2O and a specific amount of PPh3. 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.
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source ACS Publications; MEDLINE
subjects Angiotensin Receptor Antagonists - chemical synthesis
Antihypertensive Agents - chemical synthesis
Biphenyl Compounds - chemistry
Catalysis
Chelating Agents - chemistry
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings
Humans
Losartan - chemical synthesis
Magnetic Resonance Spectroscopy
Organic chemistry
Organometalloidal and organometallic compounds
P derivatives
Peptides
Preparations and properties
Ruthenium
Tetrazoles - chemical synthesis
Tetrazolium Salts - chemical synthesis
Valine - analogs & derivatives
Valine - chemical synthesis
Valsartan
title Synthesis of Angiotensin II Receptor Blockers by Means of a Catalytic System for C–H Activation
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