Sanofi

Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Astra Aktiebolag

Sanofi-Synthelabo

Aktiebolaget Astra

Csaba Huszar

Attila Nemeth

Antal Friesz

Karoly Ban

Ferenc Sperber

Eva Somfai

Dezso Korbonits

Pal Kiss

Gergely Heja

Endre Palosi

Ida Szvoboda Nee Kanzel

Csaba Gonczi

Laszlo Ledniczky

Erzsebet Szalay

Erzsebet Molnar Nee Bako

Istvan Bone

Ferenc Morasz

Gyorgy Mihalovics

Karol Gyure

Erzsebet Szabo Nee Kardos

Sandor Garaczy

Lajosne Pali

Attila Kis-Tamas

Antal Gajary

Arpad Kvari

Annamaria Ban

Marta Kruppa

Mihaly Su

Ildiko Buttkai

Iren Pali Nee Ivanics

Iidiko Buttkai

Arpad K Vari

Peter Gy Ri

Mihaly Sut

Peter Gyri

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)&#x2014;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&#x2014;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. 

Process for preparation of dronedarone by mesylation

The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some hovel intermediary compounds and the preparation thereof. 

Reductive amination process for preparation of dronedarone using amine intermediary compound

The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I: and pharmaceutically acceptable salts thereof wherein the acyl group of the benzofuran derivative of the general formula II: where R represents Calkyl-, Calkoxy- or aryl group, is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.

Process for the preparation of dronedarone

Process for the preparation of imidazolones

Process for the preparation of 4-methyl-5-(2-chloroethyl)-thiazole and

The present invention relates to a process for the preparation of compounds of general formula (I), wherein R stands for a straight chained C.sub.1-5 alkyl group substituted by a chlorine atom in the 2-position, and acid addition salts thereof, characterized by reacting a 3,5-dichloro-2-alkanone of general formula (V), wherein R is a defined above, with an inorganic thiocyamate, and a) converting the 3-thiocyanato-5-chloro-2-alkanone of general formula (IV), thus obtained, wherein R is as defined above, into 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole of general formula (II), wherein R is as defined above, by gaseous hydrochloric acid in an organic solvent, hydrogenating the said compound in the presence of a metal catalyst in an organic solvent, or b) reacting said compound of general formula (IV) with an aqueous mineral acid and treating the 2-hydroxy-4-methyl-5-(2-chloroalkyl)-thiazole of general formula (III), thus obtained with a halogenating agent, and hydrogenating the 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole of general formula (II) thus obtained, wherein R is as defined above, in an organic solvent in presence of a metal catalyst, and optionally converting the 4-methyl-5-(2-chloroalkyl)-thiazole of general formula (I), wherein R is as defined above, thus obtained or a hydrochloride salt thereof, in a manner known per into another acid addition salt or setting free a compound of general formula (I), wherein R is a defined above, from its acid addition salt.

A process is disclosed for the preparation of a compound of the Formula (VI) ##STR1## wherein X is a hydrogen atom, or OH,

Process for preparing alpha-amino-phenylacetic acid-trifluoromethane

The present invention is directed to the preparation of benzimidazole derivatives of the formula (I), ##STR1## wherein A=stands for S, SO or SO.sub.2,

Chemical process for the preparation of pharmaceutically active compounds

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Budapest, Hungary

Csaba Huszar