丙酮酸-1-^(13)C的合成研究

Synthetic Studies Toward[1-^(13)C]Pyruvate

磁共振成像(magnetic resonance imaging,MRI)因其灵敏度低而临床应用受限,超极化技术通过增强分子MRI信号克服这一限制。目前,丙酮酸-1-^(13)C是最主要的超极化生物探针,被广泛应用于超极化MRI研究。本研究以13 CO_(2)为标记原料,通过格氏试剂亲核加成反应和臭氧化反应的“两步法”合成丙酮酸-1-^(13)C,合成收率为71.5%,产品纯度>98%;同时对臭氧化反应进行调控,实现“一锅法”合成丙酮酸-1-^(13)C的方法,合成收率为70.5%,产品纯度>98%。丙酮酸-1-^(13)C的合成可为开展磁共振成像研究提供支持。

Magnetic resonance imaging(MRI)is limited in clinical application due to its low sensitivity.Hyperpolarization technology overcomes this limitation by enhancing molecular MRI signal.At present,[1-^(13)C]pyruvate is the most important hyperpolarized biological probe,which is widely used in hyperpolarized MRI research.In this study,an efficient two-step sequence of nucleophilic addition reaction and ozonation reaction for synthesis of[1-^(13)C]pyruvate from 13 CO 2 was developed,with the yield of 71.5%,and the chemical purity was above 98%.Furthermore,the ozonation reaction was optimized to furnish the one-pot synthesis of[1-^(13)C]pyruvate in 70.5%yield,and the chemical purity was above 98%.The synthesis of[1-^(13)C]pyruvate provides a basis for the development of magnetic resonance imaging research.