丙酮酸-1-^(13)C的合成研究  

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

作　　者：卿晶 贾雪雷 陈凯 代德胜 李国威 QING Jing;JIA Xuelei;CHEN Kai;DAI Desheng;LI Guowei(Shenzhen Zhonghe Headway Bio-Sci&Tech Co.,Ltd.,Shenzhen 518057,China)

机构地区：[1]深圳市中核海得威生物科技有限公司,广东深圳518057

出　　处：《同位素》2023年第2期137-143,I0002,共8页Journal of Isotopes

摘　　要：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.

关 键 词：磁共振成像 超极化 丙酮酸-1-^(13)C 亲核加成反应 臭氧化反应 

分 类 号：TL99[核科学技术—核技术及应用] O628.21[理学—有机化学]