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同位素示踪技术广泛应用于药物代谢动力学中。小分子化合物Stemazole能够促进成体干细胞增殖。为对Stemazole进行药物代谢分析,我们对其进行了定位氚标记。采用催化卤素-氚置换反应制备了氚化Stemazole药物。操作方法如下:以Br-Stemazole为反应前体,10%Pd-C为催化剂,N,N-二甲基甲酰胺为反应溶剂,在1.01×105Pa氚压下氚化反应2h;将反应混合物过滤浓缩,HPLC纯化;
Isotope tracer technology is widely used in pharmacokinetics. Small molecule compounds Stemazole can promote adult stem cell proliferation. To perform pharmacokinetic analysis of Stemazole, we mapped tritium labels. Tritiated Stemazole was prepared by catalytic halogen-tritium exchange reaction. The operation method is as follows: Br-Stemazole as a reaction precursor, 10% Pd-C as a catalyst, N, N-dimethylformamide as a reaction solvent, tritiated at 1.01 × 105Pa tritium pressure reaction 2h; the reaction mixture was filtered Concentrated, purified by HPLC;