Conway T, Diksic M
McConnell Brain Imaging Centre, Montreal Neurological Institute and Hospital, Quebec, Canada.
Int J Rad Appl Instrum A. 1991;42(5):441-6. doi: 10.1016/0883-2889(91)90103-8.
Carbon-11-labeled HECNU [1-(2-chloroethyl)-1-nitroso-3-(2-hydroxyethyl) urea] a potential chemotherapeutic agent, has been prepared by the nitrosation of the corresponding carbon-11-labeled urea, HECU, [1-(2-chloroethyl)-3-(2-hydroxyethyl) urea]. The isometric byproduct of nitrosation, 1-(2-chloroethyl)-3-nitroso-3-(2-hydroxyethyl) urea can be efficiently removed by preparative scale HPLC on a Partisil column. (11C)-HECU was prepared by reacting ethanolamine with (11C)-2-chloroethyl-isocyanate which was itself prepared by reacting [11C)-phosgene with 2-chloroethylamine hydrochloride suspended in dioxane at 60-65 degrees C. This synthesis yielded (11C)-HECNU with an average radiochemical purity of 98% in an average radiochemical yield of 18% relative to the radioactivity measured at the end of the 11C-phosgene introduction.
碳-11标记的HECNU[1-(2-氯乙基)-1-亚硝基-3-(2-羟乙基)脲]，一种潜在的化疗药物，是通过相应的碳-11标记的脲HECU[1-(2-氯乙基)-3-(2-羟乙基)脲]的亚硝化反应制备的。亚硝化反应的等规副产物1-(2-氯乙基)-3-亚硝基-3-(2-羟乙基)脲可以通过在Partisil柱上进行制备规模的高效液相色谱法有效去除。(11C)-HECU是通过使乙醇胺与(11C)-2-氯乙基异氰酸酯反应制备的，而(11C)-2-氯乙基异氰酸酯本身是通过使[11C)-光气与悬浮在二氧六环中的2-氯乙胺盐酸盐在60-65℃下反应制备的。该合成方法得到的(11C)-HECNU平均放射化学纯度为98%，相对于在11C-光气引入结束时测得的放射性，平均放射化学产率为18%。
