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글리코피롤레이트의 합성방법 및 이 활성성분을 함유하는 약학적 조성물의 제조방법
专利权人:
发明人:
김동진,구창휘,박성용,박재용,조일희,이성배,황호석
申请号:
KR1020110046537
公开号:
KR1013179240000B1
申请日:
2011.05.17
申请国别(地区):
KR
年份:
2013
代理人:
摘要:
invention anticholinergics (Anticholinergics) as effective and people excessive sweating symptoms (excessive sweating occurs) and excessive salivation (drooling), preoperative bunbisaem adjusting injection, has been recently used in endoscopic surgery face (face) hyperhidrosis drug glycosides pyrrole rate (Glycopyrrolate, Chemical name: 3-Hydroxy-1,1-dimethylpyrrolidinium bromide alpha- cyclopentylmandelate, CAS No. 596-51-0) and relates to the efficient synthesis of a derivative thereof. The pharmacological action of the glycosides found in the pyrrole rate is diversified by expanding its use by date of patent Jim has also developed a synthesis of the substance and the form of the drug is still in development. The subject matter of the present invention is 3 steps or 4 steps before synthesis (Total synthesis) as one would shorten the synthesizing step in the synthesis without going through a step consisting of methyl or an alkyl ester derivative of a conventional synthetic method effectively Mitsunobu reaction (Mitsunobu) conditions (conditions ) by improving and applying the recently developed reagents which will maximize the yield than the conventional synthetic methods, and simplifies the process of high purity and quality were obtained. In addition, by using a foreign matter more innovative safety and pollution, the local body (in particular, the side, Axilla) not at all, to develop a pressure-type nitrogen-filled aerosol spray type device than the conventional aerosol formulation was applied to the invention the formulation.본 발명은 항콜린제(Anticholinergics)로서 효과가 있고 사람들에게 과도한 발한현상(땀발생과다)과 타액분비 과다(침흘림), 수술 전 분비샘 조절용 주사제, 내시경 시술 시에 사용하고 있으며 최근 안면(얼굴) 다한증 치료제인 글리코피롤레이트(Glycopyrrolate, 화학명:3-Hydroxy-1,1-dimethylpyrrolidinium bromide alpha-cyclopentylmandelate, CAS No. 596-51-0)와 그 유도체의 효과적 합성법에 관한 것이다. 이 글리코피롤레이트의 약리작용이 다각적으로 밝혀짐으로 그 용도가 특허 등 확대일로에 있으며 또한 이 물질의 합성법이 개발되고 약제의 형태가 계속 개발되고 있다. 본 발명의 요지는 3단계 또는 4단계 전 합성(Total synthesis)으로 이루어지는 합성단계에서 효과적 합성법으로 에스테르의 메틸 또는
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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