Novel one-pot one-step synthesis of 2′[18F]fluoroflumazenil (FFMZ) for benzodiazepine receptor imaging
Novel one-pot one-step synthesis of 2′[18F]fluoroflumazenil (FFMZ) for benzodiazepine receptor imaging
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DOI：
10.1016/s0969-8051(03)00030-1
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发表时间：
2003-07-01
影响因子：
3.1
通讯作者：
Lee, MC
中科院分区：
文献类型：
--
作者：
Yoon, YH;Jeong, JM;Lee, MC
我们描述了2 '-[F-18]氟氟马西尼（FFMZ）的合成，其不同于用于苯二氮卓受体成像的通常使用的[F-18]氟乙基氟马西尼（FEFMZ）。对于一锅一步标记，前体2 '-甲苯磺酰氧基氟马西尼（TFMZ）和2'-甲磺酰氧基氟马西尼（MFMZ）分三步合成。前体成功地用无载体添加的F-18-氟化物标记，其通过与Kryptofix 2.2.2/碳酸钾的MeCN溶液。建立了[F-18]FFMZ标记和纯化的自动化系统。通过自动化系统合成后，[F-18]FFMZ的标记效率和放化纯度分别为68%和98%。磷酸化显像显示[F-18]FFMZ与大鼠中枢苯二氮卓类受体特异性结合。（C）2003 Elsevier Inc. All rights reserved.
We describe the synthesis of 2'-[F-18]fluoroflumazenil (FFMZ), which differs from the typically used [F-18]fluoroethylflumazenil (FEFMZ) for benzodiazepine receptor imaging. For one-pot one-step labeling, the precursors, 2'-tosyloxyflumazenil (TFMZ) and 2'-mesyloxyflumazenil (MFMZ), were synthesized in three steps. The precursors were successfully labeled with no-carrier-added F-18-fluoride which was activated by repeated azeotropic distillation with Kryptofix 2.2.2./potassium carbonate in MeCN. An automated system for labeling and purification of [F-18]FFMZ was developed. Labeling efficiency and radiochemical purity of [F-18]FFMZ after synthesis by the automated system were 68% and 98%, respectively. Specific binding of [F-18]FFMZ to central benzodiazepine receptor of rats was demonstrated by phosphoimaging. (C)2003 Elsevier Inc. All rights reserved.