Process for the preparation of bosentan

C - Chemistry – Metallurgy – 07 – D

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C07D 239/69 (2006.01) C07D 239/52 (2006.01)

Patent

CA 2646795

A process for the preparation of 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)- 5-(2-methoxy-phenoxy)-[2,2']bipyrimidinyl-4-yl]-benzenesulfonamide, bosentan, comprising the reaction of a compound of formula (II) or a salt thereof, (see formula II) wherein Z is an optionally protected hydroxy group, with a compound of formula (III), (see formula III) in the presence of a base; and, if necessary, the removal of the hydroxy-protecting group, and/or, if desired, the conversion of a compound of formula (I) to a salt thereof, or vice versa; and novel intermediates useful for its synthesis.

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