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Citramida rasagiline, Preparation Process and Pharmaceutical composition
专利权人:
TEVA PHARMACEUTICAL INDUSTRIES LTD.
发明人:
MARINA ZHOLKOVSKY,MUHAMMAD SAFADI,ANTON FRENKEL,RAMY LIDOR-HADAS,GREGORY VERBA,RACHEL COHEN,MICHAL KEISAR,ELIEZER BAHAR,DANIT LICHT,KONSTANTIN ULANENKO
申请号:
ARP120103780
公开号:
AR088296A1
申请日:
2012.10.10
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Claim 1: an isolated Compound, characterized in that it has the structure of formula (1) or a Salt thereof.Claim 3: a process for preparing citramida rasagiline, characterized in that it comprises the steps of: a) mixing Citric Acid with thionyl chloride in a First Solvent under Inert atmosphere to a temperature less than 30 degrees to obtain Trimethyl Citrate; (b) MIX THE Citra To Trimethyl was obtained from step a) and a solution of NaOH in a Second Solvent at a temperatureUnder 30C for 1,2 - Dimethyl Citrate; (c) mix with 1Dimethyl 2 - which was obtained from the step (b) and thionyl chloride in a Third Solvent at a Lower temperature of 30C to obtain an oily residue; (d) MIX THE Oily residue from Step c) and a mixture of rasagiline and triethylamine in the Third Solvent at a temperature below 30C To obtain rasagiline 1 - - 23 - dimethyl citramida; and e) mixing an aqueous solution of LiOH and rasagiline 1 - dimethyl - 2.3 - citramida was obtained in the step d) a combination of solvent at a temperature below 30 degrees; and (f) to adjust the PH of the Reaction mixture from step (e) with an acid to obtain 1 - citramida of rasagil Ina.Claim 9: a Pharmaceutical composition which comprises rasagiline or a pharmaceutically acceptable Salt of the same citramida rasagiline, Citric Acid, or a Salt thereof, and at least a pharmaceutically acceptable vehicle, where the citramida rasagiline The pharmaceutical composition is present in a Greater quantity of approximately 0.03% by weightWith regard to the amount of rasagiline, based on a determination made by an hplc method, except that, if the pharmaceutical composition has at least four months since its preparation, then the temperature of the pharmaceutical composition during that period Has not exceeded the Ambient Temperature for a total period of four months or more.Reivindicación 1: Un compuesto aislado, caracterizado porque tiene la estructura de fórmula (1), o una sal del mismo. Reivindicación 3: Un proceso para prep
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