Autor:	Ponchant, M., Galéa, H., Bottlaender, M., Coulon, C., Fuseau, C., Ottaviani, M., Crouzel, C.
Zdroj:	Journal of Labelled Compounds and Radiopharmaceuticals; November 2000, Vol. 43 Issue: 13 p1311-1320, 10p
Abstrakt:	[Tetrazoyl-¹¹C]LY202157 8 was prepared via a three step synthesis from ethyl (3S,4aR,6S,8aR)-6-bromomethyl-2-methoxycarbonyl-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylate 4. This bromo precursor was reacted with [¹¹C]hydrogen cyanide affording the corresponding [¹¹C]nitrile. Conversion to the tetrazole was achieved by treatment with azidotributyltin followed by hydrolysis with 6N hydrochloric acid at 200°C. After HPLC purification and analytical HPLC control, more than 370 MBq (10 mCi) of [tetrazoyl-¹¹C] LY202157 were obtained after an overall 60 minute synthesis time with 38% yield (EOB) and specific activity of 25.9 GBq/µmol (700 mCi/µmol). Ex vivo biological studies showed that the [tetrazoyl-¹¹C] LY202157 did not cross the brain blood barrier. Copyright © 2000 John Wiley & Sons, Ltd.
Databáze:	Supplemental Index
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