Sanofi

Sanofi-Aventis

Zsolt Dombrády

Antal Friesz

Zsolt Párkányi

Csaba Huszár

Adrienn Hegedus

Attila Supic

Mariann Csatarine Nagy

Antal Gajáry

Sándor Viktor Szabó

Mátyás Aradi

Ferenc Kovács

József Ugrics

Ferenc Bakos

István Gyöngyösi

Andrea Major

Erika Máténé Török

László Schultz

Erzsébet Szalay

József Zsiga

József Bálint

Marianna Csatáriné Nagy

Elemér Fogassy

Charles Suba

Mária Bakonyi

Tiborné Bai

Katalin Gáspár

The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof the hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. 

Process for preparation of dronedarone by removal of hydroxyl group

The invention relates to a compound of formula (II) and salts thereof. Also described herein are processes for the preparation of a compound of formula (II) and pharmaceutically acceptable salts thereof.

Process for preparation of dronedarone by N-butylation

The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof (formula I), which comprises oxidizing a compound of formula (VI), or a salt thereof and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (VI) and process for the preparation thereof. 

Process for preparation of dronedarone by oxidation of a hydroxyl group

The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof. 

Process for the preparation of dronedarone by oxidation of a sulphenyl group

The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof, which comprises reacting of compound of formula (IV) with compound of formula (VI) in a Grignard reaction, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and processes for the preparation thereof.  

Process for preparation of dronedarone by Grignard reaction

The invention relates to a process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that from the compound of formula (II). The hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. 

The invention relates to a novel process for preparation of dronedarone (I) and pharmaceutically acceptable salts thereof where the compound of formula (II) or salt thereof is reacted with a compound of formula L-(CH)&#x2014;CH(III), where L is a leaving group, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof. 

The subject of the present invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.

Process for the preparation of dronedarone

The process according to the invention relates to the preparation of 2-chloromethyl-thiophene of the formula (I). During this process thiophene is chloromethylated in the presence of one or more compounds containing keto group and optionally it is transformed into the compound of the formula (II). Compounds of formula (I) and (II) are intermediates of several pharmaceutically active ingredients.

Chloromethylation of thiophene

The subject of the present invention is the preparation of the (R)-(&#x2212;)-2-hydroxy-2-(2-chlorophenyl)acetic acid of the formula (I) by the resolution of the corresponding racemic compound by using the compounds of the general formula (II).

Resolution process for (R)-(-)-2-hydroxy-2-(2-chlorophenyl) acetic acid

The invention relates to the racemization process of the optically active [2-(2-thienyl)ethylamino](2-halogenophenyl)acetamides of general formula (VII) by using basic compounds. The resulting racemic compounds of general formula (VII) can thus be recycled into synthesis of the therapeutically useful compounds of general formula (VI).

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Budapest, Hungary

Zsolt Dombrády