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以[α-15N]甘氨酸为起始原料经7步反应合成15b-色胺,产率为45%。以制备的15Nb-色胺为原料经3步反应合成[2-15N]川芎哚,产率为22.2%。标记川芎哚经衍生化后用GC-MS测得15N丰度大于90%。结果表明,合成的标记物满足药物代谢研究的需要。
15b-tryptamine was synthesized in seven steps using [α-15N] glycine as starting material in 45% yield. The prepared [2-15N] chuanxiongodole was synthesized by 3 steps using 15Nb-tryptamine as raw material in a yield of 22.2%. Chuanxiong labeled by the derivatization of GC-MS measured 15N abundance greater than 90%. The results show that the synthetic markers meet the needs of drug metabolism research.