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New chemical and radiochemical routes to [18F]Rho6G-DEG-F, a delocalized lipophilic cation for myocardial perfusion imaging with PET
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-08-25 00:00:00 , DOI: 10.1039/c7md00326a
J. A. H. Inkster 1, 2, 3, 4, 5 , S. Zhang 1, 2, 3, 4, 5 , V. Akurathi 1, 2, 3, 4, 5 , A. Belanger 3, 4, 6 , S. Dubey 3, 4, 6 , S. T. Treves 3, 3, 4, 5, 6 , A. B. Packard 1, 2, 3, 4, 5
Affiliation  

New chemical and radiochemical syntheses are described for the preparation of [18F]Rho6G-DEG-F, an 18F-labeled analogue of the fluorescent dye rhodamine 6G, which has shown promise as myocardidal perfusion imaging agent. Tosylated precursors of [18F]Rho6G-DEG-F amenable to 18F-labeling were obtained either through a two-step synthesis from rhodamine 6G lactone (33% yield), or in one step from rhodamine 575 (64% yield), then purified by preparative C18 chromatography. Manual synthesis of [18F]Rho6G-DEG-F was achieved in a single radiochemical step from either the tosylate salt or the tosylate/formate double salt in DMSO under standard nucleophillic aliphatic 18F-fluorination conditions (K[18F]F/K2CO3/Kryptofix 2.2.2.). Incorporation of the [18F]F was found to be satisfactory (≥34% by TLC), despite the protic character of the precursor molecules. [18F]Rho6G-DEG-F was manually synthesized in final decay-corrected radiochemical yields of 11–26% (tosylate salt) and 9–21% (tosylate/formate double salt). The protocol was transferred to an automated synthesis unit, where the product was obtained in 3–9% radiochemical yield (n = 3) decay corrected to start-of-synthesis, >99% radiochemical purity, and a molar activity of 122–267 GBq μmol−1 (3.3–7.2 Ci μmol−1).

中文翻译:

[ 18 F] Rho6G-DEG-F的新化学和放射化学路线,这是一种用于PET心肌灌注成像的离域亲脂性阳离子

描述了用于制备[ 18 F] Rho6G-DEG-F的新化学和放射化学合成,这是荧光染料若丹明6G的18 F标记类似物,已显示出作为心肌灌注成像剂的希望。通过罗丹明6G内酯的两步合成法(产率33%)或从罗丹明575的一步法(产率64%)获得适于18 F标记的[ 18 F] Rho6G-DEG-F的甲苯磺酸化前体,然后通过制备型C 18色谱法纯化。[ 18 F] Rho6G-DEG-F的手动合成是在标准的亲核脂肪族化合物18中,由DMSO中的甲苯磺酸盐或甲苯磺酸盐/甲酸盐复盐在一个单一的放射化学步骤中完成的。F-氟化条件(K [ 18 F] F / K 2 CO 3 / Kryptofix 2.2.2)。的[掺入18 F]˚F -被认为是满意的(通过TLC≥34%),尽管前体分子的质子字符。[ 18 F] Rho6G-DEG-F是人工合成的,最终经衰变校正后的放射化学产率为11–26%(甲苯磺酸盐)和9–21%(甲苯磺酸盐/甲酸盐复盐)。将实验方案转移至自动合成装置,在该装置中,产物以3–9%的放射化学收率(n = 3)衰减,校正为合成开始,> 99%的放射化学纯度,摩尔活度为122–267吉贝微摩尔-1(3.3-7.2次微摩尔-1)。
更新日期:2017-09-04
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