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一种用于用[11C]一氧化碳进行放射性示踪剂合成的遥控高压反应器。

A remote-controlled high pressure reactor for radiotracer synthesis with [11C]carbon monoxide.

作者信息

Hostetler Eric D, Burns H Donald

机构信息

Merck Research Laboratories, PO Box 4 WP44C-2, West Point, Pennsylvania 19486, USA.

出版信息

Nucl Med Biol. 2002 Nov;29(8):845-8. doi: 10.1016/s0969-8051(02)00347-5.

Abstract

[11C]Carbon monoxide is a versatile building block for the synthesis of PET radiotracers. However, the difficulty of trapping [11C]CO in a small solvent volume has limited its utility. We wish to report the details of a simple, remotely operated High Pressure Reactor (HiPR) system for trapping and reacting practical quantities of [11C]CO. All parts used in the HiPR are commercially available, providing an inexpensive and easily assembled system. A number of compounds have been synthesized using the HiPR via palladium mediated reactions with [11C]CO, an aryl halide, and a nucleophile dissolved in dioxane. For example, AMPA receptor modulator [11C]CX546 was synthesized from its respective precursors in 37% isolated yield, uncorrected from trapped [11C]CO.

摘要

[11C]一氧化碳是用于合成正电子发射断层显像(PET)放射性示踪剂的一种多功能基础原料。然而,在小溶剂体积中捕获[11C]CO的困难限制了其应用。我们希望报告一种简单的远程操作高压反应器(HiPR)系统的详细情况,该系统用于捕获和反应实际量的[11C]CO。HiPR中使用的所有部件均可从市场购得,提供了一个廉价且易于组装的系统。已经使用HiPR通过钯介导的反应,将[11C]CO、芳基卤化物和亲核试剂溶解在二氧六环中,合成了多种化合物。例如,AMPA受体调节剂[11C]CX546由其各自的前体合成,分离产率为37%,未对捕获的[11C]CO进行校正。

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