Sanofi-aventis

Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

József Ugrics

Eva Somfai

Zsolt Dombrády

Attila Supic

Zsolt Párkányi

Istvan Jelinek

Istvan Turcsan

Mátyás Aradi

Ferenc Kovács

Antal Gajáry

Sándor Viktor Szabó

Andrea Major

Iren Csaszar Nee Toth

Erika Máténé Török

Ferenc Bakos

László Schultz

Istvan Csik

Erzsébet Szalay

István Gyöngyösi

József Zsiga

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

In the production of perparine or papaverine and their hydrochlorides, the formation of impurities in the reaction mixture is suppressed by fractionating a 3,4-di-R-benzyl-cyanide in the presence of an organic base (e.g. pyridine, dimethylformamide, ethylenediamine or triethylamine) followed by hydrogenation with a Raney-nickel catalyst treated with aqueous ammonium carbonate solution. R is methoxy or ethoxy.

Process for the manufacture of pure isoquinoline derivatives

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Budapest, Hungary

József Ugrics