Tremblay Sébastien, Ouellet René, Rodrigue Serge, Langlois Réjean, Bénard François, Cunnane Stephen C
Research Center on Aging, Sherbrooke University Geriatric Institute, 1036 Belvedere Street South, Sherbrooke, Québec, Canada J1H 4C4.
Appl Radiat Isot. 2007 Aug;65(8):934-40. doi: 10.1016/j.apradiso.2007.03.015. Epub 2007 Mar 28.
An automated, one-pot radio-synthesis module for the routine preparation of 1-[(11)C]acetoacetic acid has been developed. The enolate anion of acetone was reacted with [(11)C]CO(2) in tetrahydrofuran (THF), followed by hydrolysis and purification by ion-exchange chromatography. The total synthesis time was 18 min and radiochemical yield was 34% after decay correction. HPLC analysis showed < or =3% impurities while residual THF (< or =200 ppm) and ethanol (< or =500 ppm) were well under the tolerable limits for human studies.
已开发出一种用于常规制备1-[(11)C]乙酰乙酸的自动化单步放射性合成模块。丙酮的烯醇负离子在四氢呋喃（THF）中与[(11)C]CO(2)反应，随后进行水解并通过离子交换色谱法纯化。总合成时间为18分钟，衰变校正后的放射化学产率为34%。高效液相色谱分析显示杂质含量≤3%，而残留的THF（≤200 ppm）和乙醇（≤500 ppm）远低于人体研究的可耐受限度。
