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Synthesis 1996; 1996(11): 1325-1330
DOI: 10.1055/s-1996-4383
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Synthesis of the Imidazole-Derived AT1-Selective ANG II Receptor Antagonist HR 720 Utilizing Reductive Amination as Key Step

Holger Heitsch1 , Adalbert Wagner, Neerja Yadav-Bhatnagar2 , Christine Griffoul-Marteau
  • 1HOECHST AG, HMR TA Cardiovascular Agents, G 838, D-65926 Frankfurt/Main, Germany, Fax +49(69)30581551; E-mail heitsch@msmrd.frankfurt.hoechst-ag.d400.de
  • 2ROUSSEL UCLAF, 102 Route de Noissy, F-93235 Romainville Cedex, France
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Publication Date:
31 December 2000 (online)

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The straightforward synthesis of the (1-methylbiphenylsulfonyl)-urea substituted imidazole HR 720, an orally active ANG II receptor antagonist, by reductive amination of 2’-sulfonamidobiphenylcarbaldehydes, derived from Suzuki-type phenyl-phenyl coupling procedures, as key step is described.

Suzuki coupling - reductive amination - cyclodehydration - imidazoles - biphenylsulfonylureas and -carbamates