碳-11标记甘氨酸以及二肽L-苯丙氨酰甘氨酸和L-亮氨酰甘氨酸的合成。

Synthesis of carbon-11 labelled glycine and the dipeptides L-phenylalanylglycine and L-leucylglycine.

作者信息

Bolster J M, Vaalburg W, Elsinga P H, Woldring M G, Wynberg H

出版信息

Int J Rad Appl Instrum A. 1986;37(9):985-7. doi: 10.1016/0883-2889(86)90251-0.

Abstract

Carbon-11 labelled glycine has been prepared in 30 min by carboxylation of alpha-lithiomethylisocyanide with a radiochemical yield of 10-15%. After coupling with L-phenylalanine-N-carboxyanhydride and L-leucine-N-carboxyanhydride followed by HPLC purification, the corresponding dipeptides were obtained in 20 min with a radiochemical yield of 30-40%. Consequently, starting with 11CO2, non carrier added L-phenylalanyl[1-(11)C]glycine and L-leucyl-[1-(11)C]glycine in 0.1 N NaH2PO4 were obtained in 50 min with a radiochemical yield of 3-6%. The radiochemical yield figures are not corrected for decay.

摘要

通过用α-锂代甲基异氰化物进行羧化反应，在30分钟内制备出了碳-11标记的甘氨酸，其放射化学产率为10%-15%。在与L-苯丙氨酸-N-羧基酐和L-亮氨酸-N-羧基酐偶联，随后通过高效液相色谱法纯化后，在20分钟内获得了相应的二肽，放射化学产率为30%-40%。因此，以11CO₂为起始原料，在50分钟内获得了未添加载体的0.1N NaH₂PO₄中的L-苯丙氨酰基[1-(11)C]甘氨酸和L-亮氨酰基-[1-(11)C]甘氨酸，放射化学产率为3%-6%。放射化学产率数据未进行衰变校正。