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Synthesis of radiolabeled styrylpyridines with 18F from tosylate precursors and stable pharmaceutical compositions thereof
- 专利权人:
- Avid Radiopharmaceuticals; Inc.
- 发明人:
- BENEDUM, Tyler,GOLDING, Geoff,LIM, Nathaniel,ZHANG, Wei
- 申请号：
- ES09837135
- 公开号：
- ES2620402T3
- 申请日:
- 2009.12.29
- 申请国别(地区):
- ES
- 年份:
- 2017
- 代理人:
- 摘要：
- A method of producing a radiopharmaceutical composition for imaging neurodegenerative diseases of the brain by positron emission tomography (PET) comprising: an effective amount of ((E) -4- (2- (6- (2- ( 2- (2- [18 F] fluoroethoxy) ethoxy) ethoxy) pyridin-3-yl) vinyl) -N-methylbenzenamine)； 10.0% (v / v) ethyl alcohol； and 0.5% (w / v) of sodium ascorbate, in 0.9% (w / v) of aqueous sodium chloride, in which the process comprises the steps of: preparing a vinylaniline compound protected with Boc mono； converting the vinylaniline compound into a methyl carbamate derivative, t-butyl； react 2-halo 5-iodopyridine with triethylene glycol； reacting the methyl carbamate derivative, t-butyl with the compound resulting from the reaction step of 2-halo 5-iodopyridine with triethylene glycol to produce (E) -terc-butyl 4- (2- (6- (2- (2- (2-) (2- (2-hydroxyethoxy) ethoxy) ethoxy) pyridin-3-yl) vinyl) phenyl (methyl) carbamate； and reacting the (E) -terc-butyl 4- (2- (6- (2- (2- (2- (2-hydroxyethoxy) ethoxy) ethoxy) pyridin-3-yl) vinyl) phenyl (methyl) carbamate with chloride of tosyl to form (E) -2- (2- (2- (5- (4- (tert-butoxycarbonyl (methyl) amino) styryl) pyridin-2-yloxy) ethoxy) ethoxy) ethyl 4-methylbenzene sulfonate； React (E) -2- (2- (2- (5- (4- (tert-butoxycarbonyl (methyl) amino) styryl) pyridin-2-yloxy) ethoxy) ethoxy) ethyl 4-methylbenzene sulfonate and an ion fluoride [18F] in dimethylsulfoxide solution (DMSO) or high-boiling aprotic solvent to produce (E) -4- (2- (6- (2- (2- (2- (2- [18F] fluoroethoxy) ethoxy)) ethoxy ) pyridin-3-yl) vinyl) -N-methylbencenamine)； isolate (E) -4- (2- (6- (2- (2- (2- [18 F] fluoroethoxy) ethoxy) ethoxy) pyridin-3-yl) vinyl) -N-methylbenzenamine)； purify the (E) -4- (2- (6- (2- (2- (2- [18 F] fluoroethoxy) ethoxy) ethoxy) pyridin-3-yl) vinyl) -N-methylbenzenamine)； and formulate (E) -4- (2- (6- (2- (2- (2- [18 F] fluoroethoxy) ethoxy) ethoxy) pyridin-3-yl) vinyl) -N-methylbenzenamine) in a solution aqueous sodium chloride-0.9% ethyl
- 来源网站：
- 中国工程科技知识中心
- 来源网址：
- http://www.ckcest.cn/home/
