PROCESS FOR THE INDUSTRIAL SYNTHESIS OF TETRAESTERS OF 5-BIS(CARBOXYMETHYL)AMINO-3-CARBOXYMETHYL-4-CYANO-2-THIOPHENECARBOXYLIC ACID, AND APPLICATION TO THE SYNTHESIS OF BIVALENT SALTS OF RANELIC ACID AND THEIR HYDRATES

摘要

A PROCESS FOR THE INDUSTRIAL SYNTHESIS OF A COMPOUND OF FORMULA (I) IS DISCLOSED. IN THE FORMULA I ,R AND R’,WHICH ARE THE SAME OR DIFFERENT,EACH REPRESENT LINEAR OR BRANCHED (C1-C6)ALKYL,WHEREIN A COMPOUND OR FORMULA (III): WHEREIN R IS AS DEFINED HEREINBEFORE,IS REACTED WITH A COMPOUND OF FORMULA (IV): WHEREIN R’ IS AS DEFINED HEREINBEFORE,IN THE PRESENCE OF A CATALYTIC AMOUNT OF A C8-C10 TYPE QUATERNARY AMMONIUM COMPOUND,AND IN THE PRESENCE OF POTASSIUM CARBONATE,AT IS THEN CONCENTRATED BY DISTILLATION;A CO-SOLVENT IS THEN ADDED,AND THE REACTION MIXTURE IS COOLED AND FILTERED TO YIELD,AFTER DRYING OF THE POWDER THREBY OBTAINED,THE COMPOUND OF FORMULA (I),IT BEING UNDERSTOOD THAT A C8-C10 TYPE QUATERNARY AMMONIUM COMPOUND IS A COMPOUND OF FORMULA (A) OR A MIXTURE OF COMPOUNDS OF FORMULA (A): R1R2R3R4-N+-X WHEREIN R1 REPRESENTS (C1-C6)ALKYL,R2,R3,AND R4, WHICH ARE IDENTICAL OR DIFFERENT,EACH REPRESENT (C8-C10)ALKYL,AND X REPRESENTS HALOGEN.