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[用¹⁰³Ru和¹⁰³mRh标记后,氟哌啶醇合成及器官分布中的二茂铁、二茂钌和二茂铑类似物]

[Ferrocene, ruthenocene and rhodocene analogs in haloperidol synthesis and organ distribution after labeling with 103Ru and 103mRh].

作者信息

Wenzel M, Wu Y

机构信息

Pharmazeutisches Institut, Freie Universität Berlin, Berlin-Dahlem, Deutschland.

出版信息

Int J Rad Appl Instrum A. 1988;39(12):1237-41. doi: 10.1016/0883-2889(88)90106-2.

Abstract

Ferrocene-Haloperidol was synthesized by N-alkylation of 4-(4'-chlorophenyl)- 4-hydroxypiperidine with 1-ferrocenyl-4-chlor-butan-1-on. By heating the ferrocene-haloperidol with 103RuCl3 the 103Ru-labelled ruthenocene-haloperidol was obtained. This compound showed a high affinity for lung but not for brain in rats and mice. The decay of the 103Ru labelled compound results in the formation of the 103mRh labelled rhodocene-haloperidol, which is rapidly oxidized by air to the corresponding rhodocinium-haloperidol. This compound can be separated by extraction and TLC.

摘要

二茂铁-氟哌啶醇由4-(4'-氯苯基)-4-羟基哌啶与1-二茂铁基-4-氯丁-1-酮进行N-烷基化反应合成。将二茂铁-氟哌啶醇与103RuCl3加热,得到103Ru标记的钌茂-氟哌啶醇。该化合物在大鼠和小鼠体内对肺有高亲和力,但对脑无亲和力。103Ru标记化合物的衰变导致形成103mRh标记的铑茂-氟哌啶醇,其会被空气迅速氧化为相应的铑鎓-氟哌啶醇。该化合物可通过萃取和薄层色谱法分离。

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