专利号:WO-2011016738-A8 优先权日:2009-08-05 标 题 :A process for the synthesis of 1-hydroxy-3-(n-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate 发明人:SZULC MARCIN; SLISEWSKI TOMASZ; DEMBKOWSKI LESZEK; JASTRZEBSKA BEATA; RACHON JANUSZ; MAKOWIEC SLAWOMIR 权利人:ZAKLADY FARMACEUTYCZNE POLPHARMA SA; POLITECHNIKA GDANSKA; SZULC MARCIN; SLISEWSKI TOMASZ; DEMBKOWSKI LESZEK; JASTRZEBSKA BEATA; RACHON JANUSZ; MAKOWIEC SLAWOMIR 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.
专利号:WO-2008058722-A1 优先权日:2006-11-16 标 题:Reagent and use thereof for the production of bisphosphonates 发明人:LERSTRUP KNUD; PREIKSCHAT HERBERT FRITZ; FISCHER ERIK 权利人:SANDOZ AS; LERSTRUP KNUD; PREIKSCHAT HERBERT FRITZ; FISCHER ERIK 摘要:A new liquid reagent is disclosed in form of an ionic liquid containing phosphorous acid and a tertiary amine. The reagent can be used as a replacement of phosphorous acid, where the new reagent as a liquid reagent can be handled using usual equipment for handling liquids and the dosing of the reagent can therefore be controlled more precisely in industrial plants compared to phosphorous acid, which is a solid at ambient temperature. The new liquid reagent is particular suitable for the synthesis of bisphosphonates.
专利号:WO-2011016738-A1 优先权日:2009-08-05 标 题:A process for the synthesis of 1-hydroxy-3-(n-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate
专利号:US-2010228052-A1 优先权日:2006-06-23 标 题:Process for the synthesis of ibandronate sodium
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合成参考文献
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