摘要 |
A process for the synthesis of 1-hydroxy-3-(N-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate which consists in the reaction of phosphorus trichloride with an aqueous solution of 3-(N-methylpentylamino)propionic acid hydrochloride at a temperature of 0-80°C, removing excess unreacted phosphorus trichloride, hydrolysis of the reaction mixture under reflux, conversion of 1-hydroxy-3-(N- methylpentylamino) propylidene bisphosphonic acid into its monosodium salt using sodium cation-containing alkaline substances, crystallisation using an anti-solvent. Also disclosed is a process for the synthesis of a polymorphic form of 1-hydroxy-3-(N-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate which consists of initiating and carryout the crystallisation using acetone at a temperature of 0-5°C.
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申请人 |
ZAKLADY FARMACEUTYCZNE POLPHARMA SA;POLITECHNIKA GDANSKA;SZULC, MARCIN;SLISEWSKI, TOMASZ;DEMBKOWSKI, LESZEK;JASTRZEBSKA, BEATA;RACHON, JANUSZ;MAKOWIEC, SLAWOMIR |
发明人 |
SZULC, MARCIN;SLISEWSKI, TOMASZ;DEMBKOWSKI, LESZEK;JASTRZEBSKA, BEATA;RACHON, JANUSZ;MAKOWIEC, SLAWOMIR |