Dipharma S.p.a.

Lundbeck Pharmaceuticals, Italy

Mauro Ercoli

Gabriele Razzetti

Graziano Castaldi

Pietro Allegrini

Domenico Magrone

Novel phenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists and the processes for the conversion thereof to biologically active molecules.

Phenyltetrazole compounds

A process for the preparation of a compound of formula (I), or a salt thereof wherein R is H, C-Calkyl, aryl or aryl-C-Calkyl; comprising the reaction between a compound of formula (II) wherein Rand Rare independently hydrogen, C-Calkyl, aryl, aryl-C-Calkyl, or Rand R, taken together, form a &#x2014;(CH)&#x2014;V&#x2014;(CH)&#x2014; group, in which V is NRor C(R)wherein Ris hydrogen, C-Calkyl, aryl or aryl-C-Calkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) in which Rand Rare independently C-Calkyl, aryl or aryl-C-Calkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C-Calkyl, aryl or aryl-C-Calkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

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Milan, Italy

Mauro Ercoli