Synthesis of [11C-carbonyl]hydroxyureas by a rhodium-mediated carbonylation reaction using [11C]carbon monoxide
Synthesis of [11C-carbonyl]hydroxyureas by a rhodium-mediated carbonylation reaction using [11C]carbon monoxide
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DOI：
10.1002/jlcr.1062
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发表时间：
2006-04-01
影响因子：
1.8
通讯作者：
Langstrom, Bengt
中科院分区：
文献类型：
--
作者：
Barletta, Julien;Karimi, Farhad;Langstrom, Bengt
已成功使用低浓度[C-11]一氧化碳标记[C-11]羟基脲。衰变校正的放射化学产率为38 +/-3%，[C-11]一氧化碳的捕获效率为90 +/-5%。该合成通过铑介导的羰基化反应进行，该羰基化反应从叠氮基三甲基硅烷开始，并且铑络合物由氯（1，5-环辛烷基）铑（I）二聚体（[Rh（cod）C] 1,2）和1，2-双（二苯基膦基）乙烷（dppe）原位制备。(13 C）使用该方法合成羟基脲，并通过C-13-NMR确认标记的位置。为了进行准确的LC-MS鉴别，以35 +/- 4%的衰变校正放射化学产率合成了衍生物1-羟基-3-苯基[C-11]脲。在13 μ A/h轰击和21分钟合成后，从6.75 GBq的[C-11]一氧化碳开始收集1.6 GBq的纯1-羟基-3-苯基[C-11]脲，该化合物的比放射性为686 GBq/μ mol（总质量为3.47 nmol）。[C-11]羟基脲可与PET结合使用，以评估个体患者肿瘤组织对该抗癌剂的吸收。版权所有（c）2006约翰威利父子有限公司。
[C-11]Hydroxyurea has been successfully labelled using [C-11]carbon monoxide at low concentration. The decay-corrected radiochemical yield was 38 +/- 3%, and the trapping efficiency of [C-11]carbon monoxide in the order of 90 +/- 5%. This synthesis was performed by a rhodium-mediated carbonylation reaction starting with azidotrimethylsilane and the rhodium complex being made in situ by chloro(1,5-cyclooctadiene)rhodium(l) dimer ([Rh(cod)C]12) and 1,2-bis(diphenylphosphino)ethane (dppe). (13 C)Hydroxyurea was synthesized using this method and the position of the labelling was confirmed by C-13-NMR. In order to perform accurate LC-MS identification, the derivative 1-hydroxy-3-phenyl[C-11]urea was synthesized in a 35 +/- 4% decay-corrected radiochemical yield. After 13 mu A h bombardment and 21 min synthesis, 1.6 GBq of pure 1-hydroxy-3-phenyl[C-11]urea was collected starting from 6.75 GBq of [C-11]carbon monoxide and the specific radioactivity of this compound was in the order of 686 GBq/mu mol (3.47 nmol total mass). [C-11]Hydroxyurea could be used in conjunction with PET to evaluate the uptake of this anticancer agent into tumour tissue in individual patients. Copyright (c) 2006 John Wiley & Sons, Ltd.