Egan Judith A, Laseter Anne G, Filer Crist N
PerkinElmer Life Sciences, Inc., 549 Albany St., Boston, MA 02118, USA.
Appl Radiat Isot. 2002 Sep;57(3):343-5. doi: 10.1016/s0969-8043(02)00117-3.
To study its mechanism of antimalarial action, a tritium labelled analogue of (+/-)-chloroquine was required at high specific activity. Two synthetic methods were successfully employed. [3-3H] (+/-)-Chloroquine 2 was prepared by the catalytic tritium dehalogenation of an iodo precursor and [N-ethyl-3H] (+/-)-chloroquine 4 was synthesized by the alkylation of (+/-)-desethylchloroquine with [3H] ethyl iodide.
为研究其抗疟作用机制,需要高比活度的氚标记的(±)-氯喹类似物。成功采用了两种合成方法。[3-³H](±)-氯喹2是通过碘代前体的催化氚脱卤制备的,[N-乙基-³H](±)-氯喹4是通过(±)-去乙基氯喹与[³H]碘乙烷的烷基化反应合成的。