Synthesis of [2H4]oxymetazoline and [14C]oxymetazoline

被引:0
|
作者
Brugger, Michelle L. [1 ]
Borges, Scott [1 ]
Ren, Sumei [1 ]
McNamara, Paul [1 ]
机构
[1] Merck & Co Inc, Merck Res Labs, Kenilworth, NJ 07033 USA
来源
关键词
H-2(4)]oxymetazoline; C-14]oxymetazoline; Afrin; SCH; 9384; carbon-14; synthesis; AROMATIC-COMPOUNDS; BROMOMETHYLATION; ACIDS;
D O I
10.1002/jlcr.1805
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
An efficient synthesis of [H-2(4)] and [C-14]oxymetazoline has been developed. Both compounds follow the same synthetic route with the introduction of the label occurring at different synthetic steps. The synthesis of [H-2(4)]oxymetazoline from [H-2(4)]ethylene diamine was achieved in one step with a 40% yield. The synthesis of [C-14]oxymetazoline from potassium [C-14]cyanide was achieved in two steps with an overall radiochemical yield of 67%.
引用
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页码:793 / 800
页数:8
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