由松萝酸合成14C-角鲨烯的两种新的简便方法。
Two new convenient syntheses of 14C-squalene from turbinaric acid.
作者信息
Philippe Nicolas, Rivron Luc, De Bruin Béatrice, Schofield Joseph, Roy Sébastien
机构信息
Isotope Chemistry, Integrated Drug Discovery, Sanofi-Aventis R&D, Vitry-sur-Seine, France.
Pharmacokinetics, Dynamics and Metabolism, Translational Medicine and Early Development, Sanofi-Aventis R&D, Alfortville, France.
出版信息
J Labelled Comp Radiopharm. 2018 Oct;61(12):878-884. doi: 10.1002/jlcr.3672. Epub 2018 Sep 10.
Carbon-14 labeled (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene, also known as squalene, was synthesized as a tool for pharmacokinetic studies. Two simple and efficient labeling approaches were developed to give [2- C]-squalene and [3- C]-squalene from a halogenated precursor derived from turbinaric acid. They were obtained in 13.5% radiochemical yield in 6 steps and in 38% radiochemical yield in 3 steps respectively from carbon-14 labeled potassium cyanide with a radiochemical purity higher than 98% in both cases.
碳 - 14标记的（6E，10E，14E，18E）-2,6,10,15,19,23 - 六甲基二十四碳 - 2,6,10,14,18,22 - 六烯，也称为角鲨烯，被合成用作药代动力学研究的工具。开发了两种简单有效的标记方法，以从源自海绵甾酸的卤化前体生成[2 - C] - 角鲨烯和[3 - C] - 角鲨烯。它们分别以6步13.5％的放射化学产率和3步38％的放射化学产率从碳 - 14标记的氰化钾获得，两种情况下放射化学纯度均高于98％。
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