[N-甲基-¹¹C] - 舍曲林的放射性合成

The radiosynthesis of [N-methyl-11C]-sertraline.

作者信息

Lasne M C, Pike V W, Turton D R

机构信息

MRC Cyclotron Unit, Hammersmith Hospital, London, U.K.

出版信息

Int J Rad Appl Instrum A. 1989;40(2):147-51. doi: 10.1016/0883-2889(89)90190-1.

DOI:10.1016/0883-2889(89)90190-1

PMID:2541104

Abstract

[N-methyl-11C]Sertraline, a potential agent for the study of the serotonergic system in vivo with positron emission tomography, was prepared by N-methylation of the corresponding norcompound with [11C]iodomethane, which was itself prepared from cyclotron-produced [11C]carbon dioxide. Under the best conditions found [norsertraline free base (20 mM) in DMF (0.70 mL), 120 degrees C for 8 min] [N-methyl-11C]-sertraline can be prepared in 43% radiochemical yield from [11C]iodomethane (decay-corrected), corresponding to 20% overall radiochemical yield from [11C]carbon dioxide (decay-corrected), with high specific radioactivity. Preparations can be ready for i.v. injection 50 min from the end of radionuclide production.

摘要

[11C]N-甲基舍曲林是一种通过正电子发射断层扫描在体内研究血清素能系统的潜在药物，它是由相应的去甲化合物与[11C]碘甲烷进行N-甲基化反应制备而成，而[11C]碘甲烷本身是由回旋加速器产生的[11C]二氧化碳制备的。在最佳条件下（在0.70 mL N,N-二甲基甲酰胺中加入20 mM去甲舍曲林游离碱，120℃反应8分钟），由[11C]碘甲烷（经衰变校正）制备[11C]N-甲基舍曲林的放射化学产率可达43%，相当于由[11C]二氧化碳（经衰变校正）制备的总放射化学产率为20%，且具有较高的比放射性。从放射性核素生产结束起50分钟后，制剂即可用于静脉注射。