PROCESS FOR THE PREPARATION OF FUNCTIONALISED BENZOCYCLOBUTENES, AND APPLICATION IN THE SYNTHESIS OF IVABRADINE AND ADDITION SALTS THEREOF WITH A PHARMACEUTICALLY ACCEPTABLE ACID

摘要

PROCESS FOR THE PREPARATION OF COMPOUNDS OF FORMULA (IV) : WHEREIN R1 , R2 , R3 AND R4 , WHICH MAY BE IDENTICAL OR DIFFERENT, EACH REPRESENT A HYDROGEN ATOM, A LINEAR OR BRANCHED (C1 -C6 )) ALKYL GROUP, A LINEAR OR BRANCHED (C1 -C6 )) ALKOXY GROUP, A FLUORINE ATOM, A CHLORINE ATOM, A PROTECTED AMINE GROUP, A PROTECTED HYDROXYL GROUP, AN ALKOXYCARBONYL GROUP IN WHICH THE ALKOXY GROUP IS LINEAR OR BRANCHED (C1 -C6 )), OR A CF3 GROUP, OR R1 =R4 =H AND R2 AND R3 TOGETHER WITH THE CARBON ATOMS CARRYING THEM FORM A 1,3-DIOXOLANE GROUP, R5 , REPRESENTS A SATURATED OR UNSATURATED, LINEAR OR BRANCHED (C1 -C6 ))ALKYL GROUP, A LINEAR OR BRANCHED (C1 -C6 ) HYDROXYALKYL GROUP IN WHICH THE HYDROXYL FUNCTION IS PROTECTED, OR A CO2 R7 GROUP IN WHICH R7 IS A LINEAR OR BRANCHED (C1 -C6 ))ALKYL GROUP, R6 REPRESENTS A CYANO GROUP OR A CO2 R8 GROUP IN WHICH R8 IS A LINEAR OR BRANCHED (C1 -C6 )-ALKYL GROUP. APPLICATION IN THE SYNTHESIS OF IVABRADINE, ADDITION SALTS THEREOF WITH A PHARMACEUTICALLY ACCEPTABLE ACID AND HYDRATES THEREOF.