Maiti Dilip K, Chakraborty Pulak K, Chugani Diane C, Muzik Otto, Mangner Thomas J, Chugani Harry T
Department of Pediatrics, School of Medicine, PET Center, Children's Hospital of Michigan, Wayne State University, Detroit, MI 48201, USA.
Appl Radiat Isot. 2005 May;62(5):721-7. doi: 10.1016/j.apradiso.2004.10.005. Epub 2004 Nov 30.
An improved one-pot synthesis procedure for routine production of [carbonyl-(11)C]desmethyl-WAY-100635 ([(11)C]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-NaH(2)PO(4) 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/micromol (3.6-5.0 Ci/micromol, EOS, n=2) when ca. 37.0 GBq (ca. 1.0 Ci) of starting [(11)C]CO(2) was used. Unlabeled mass of [(11)C]DWAY was found to be 0.15-0.24 microg/mL and the precursor was present in less than 50 ng/mL in final production solution.
本文描述了一种用于常规生产[羰基-(11)C]去甲基-WAY-100635（[(11)C]DWAY）的改进的一锅合成方法。还开发了一种对粗产物的有效纯化方法，该方法通过使用55/45乙醇-磷酸二氢钠缓冲液（20 mM，pH = 6.5）作为洗脱剂的C-18反相半制备高效液相色谱法来完成。收集2.0 - 2.5 mL体积的所需产物馏分，并用11 mL 0.9%的生理盐水配制。放射性配体在45分钟（放化终点）即可供人体使用。产物的放化产率为11.1±1.8%（放化终点，n = 15），放化纯度>99%。当使用约37.0 GBq（约1.0 Ci）的起始[(11)C]CO₂时，比活度为133.2 - 185.0 GBq/μmol（3.6 - 5.0 Ci/μmol，放化起始点，n = 2）。[(11)C]DWAY的未标记质量为0.15 - 0.24 μg/mL，且前体在最终生产溶液中的含量低于50 ng/mL。
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