Erregierre S.p.a.

Daniele De Zani

Massimo Ferrari

Matteo Bonaldi

Paolo Belotti

Stefano Vezzosi

The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate. 

Process for the preparation of bazedoxifene

Disclosed is a process for the preparation of toltrazuril of formula (I) via the intermediate N-methyl-N'-[3-methyl-4-[4-[(trifluoromethyl)thio]phenoxy]phenyl] imidodicarbonic diamide of formula (III)  wherein intermediate (III) is obtained via a novel intermediate without the use of potentially hazardous reagents or potentially unstable intermediates.

Process for the preparation of toltrazuril and an intermediate useful for its preparation

The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.

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Roncello, Italy

Daniele De Zani