PROCESS FOR PREPARATION OF DRONEDARONE BY MESYLATION

PROCESS FOR PREPARATION OF DRONEDARONE BY MESYLATION

The invention relates to a novel process for preparation of N-[2-n-butyl-3-[4-[3-(di-n-butylamino)-propoxy]-benzoyl]-benzofuran-5-yl]methanesulfonamide (I) and pharmaceutical acceptable salts thereof, where a salt of (5-amino-2-butyl-1-benzofuran-3-yl){4-[3-(di-n-butylamino)propoxy]phenyl}methanone...

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Hauptverfasser: HUSZAR, CSABA, FRIESZ, ANTAL
Format: Patent
Sprache:eng ; fre ; ger
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator HUSZAR, CSABA
FRIESZ, ANTAL
description The invention relates to a novel process for preparation of N-[2-n-butyl-3-[4-[3-(di-n-butylamino)-propoxy]-benzoyl]-benzofuran-5-yl]methanesulfonamide (I) and pharmaceutical acceptable salts thereof, where a salt of (5-amino-2-butyl-1-benzofuran-3-yl){4-[3-(di-n-butylamino)propoxy]phenyl}methanone of formula (II)-where A is a mono- or dibasic acid forming an acid addition salt with the compound of formula (II), n is 1 if A is dibasic acid and n is 1 or 2 if A is a monobasic acid-is reacted with a mesylating reagent in a heterogen reaction, if desired, in the presence of a phase transfer catalyst. The invention also relates to the novel salts of compound of formula (II), for the preparation thereof and their use in the preparation of dronedarone.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title PROCESS FOR PREPARATION OF DRONEDARONE BY MESYLATION
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