Synthesis procedure for routine production of [carbonyl-¹¹C]desmethyl-WAY-100635

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• 作者：Maiti ; Dilip K. ; Chakraborty ; Pulak K. ; Chugani ; Diane C. ; Muzik ; Otto ; Mangner ; Thomas. J. ; et. al.
• 关键词：[carbonyl-¹¹C]Desmethyl-WAY-100635 ; 5-HT_1A receptors ; PET imaging ; 1 ; 2-Dichloroethane
• 刊名：Applied Radiation and Isotopes
• 出版年：2005
• 期刊代码：6_09698043
• 类别：ce
• 出版时间：May, 2005
• 卷：62
• 期：5
• 页码：721-727
• 文件大小：306 K

摘要

An improved one-pot synthesis procedure for routine production of [carbonyl-¹¹C]desmethyl-WAY-100635 ([¹¹C]DWAY) is described. An efficient purification of the crude product has also been developed and was accomplished by C-18 reversed-phase semi-preparative HPLC using 55/45 EtOH–NaH₂PO₄ buffer (20 mM, pH=6.5) as the eluent. The desired product fraction was collected in a 2.0–2.5 mL volume and formulated with 11 mL of 0.9%saline. The radioligand was ready for human use in 45 min (EOB). The product was obtained with a radiochemical yield of 11.1±1.8%(EOB, n=15) with a radiochemical purity of >99%. Specific activity was 133.2–185.0 GBq/μmol (3.6–5.0 Ci/μmol, EOS, n=2) when ca. 37.0 GBq (ca. 1.0 Ci) of starting [¹¹C]CO₂ was used. Unlabeled mass of [¹¹C]DWAY was found to be 0.15–0.24 μg/mL and the precursor was present in less than 50 ng/mL in final production solution.