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PROCESS FOR THE PREPARATION (6S)-(-)-5,6,7,8- TETRAHYDRO-6-[PROPYL-(-2-THIENYL) ETHYL] AMINO-1- NAPHTHOL (ROTIGOTINE)
专利权人:
发明人:
MARTA POMARES,FRANCISCO MARQUILLAS OLONDRIZ
申请号:
IN4347/DELNP/2011
公开号:
IN2011DN04347A
申请日:
2011.06.09
申请国别(地区):
IN
年份:
2012
代理人:
摘要:
(a) acetylating (S)-(-)-5-hydroxy-N-n-propyl-2-aminotetraline to afford the acetate (b) reacting this acetate, (-)-5-acetoxy- N-n-propyl-2-aminotetraline, with 2-(2-thienyl)ethanol 2- nitrobenzenesul-fonate (d) hydrolyzing (6S)-(-)-l-acetoxy-5, 6,7,8- tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-l-naphthalene to afford (6S)-(- )-5, 6, 7, 8-terrahydro-6-[propyl-(2-thienyl)ethyl]amino-l-naphthol (Rotigotine) and (d) purifying rotigotine either by the acety-lation reaction and subsequent hydrolysis of the formed acetate or by salification of rotigotine through hydrochloride or hydrobro-mide formation and subsequent base release. Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson"s disease.
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中国工程科技知识中心
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