Krka, D.d., Novo Mesto

Martin Putala

Miroslav Veverka

Heinrich Brath

Silvo Zuppancic

The invention provides a process for the preparation of a sartan derivative of formula (I) (formula as filed in paper form) (I) wherein the substituents have the meaning indicated in the description, or a pharmaceutically acceptable salt thereof, comprising reacting 2-cyanophenylboronic acid or a derivative thereof with a p-halobenzyl-1H-imidazole derivative of formula (VI), (formula as filed in paper form) (VI) wherein (part of formula as filed in paper form), X, Y, Rand Rare as defined above, and Z is I, Br or Cl, in the presence of a transition metal catalyst and an inorganic or organic base. The invention also provides new intermediates of formula (V), (formula as filed in paper form) (V) wherein M is an alkali metal or an NRRRRgroup; and of formula (II) (formula as filed in paper form) (II). 

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Bratislava, Slovakia

Martin Putala