公开(公告)号：KR1020090073659A

公开(公告)日：2009-07-03

申请号：KR1020070141668

申请日：2007-12-31

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  조정혁 ,  조남현 ,  안광일 ,  천기정 ,  이교철 ,  문병석 ,  최태현 ,  구대호

IPC: C07D405/04 ,  C07H15/22

Abstract: A manufacturing method for manufacturing a 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound is provided to produce a compound having high intake rate by specifically activating in a cell line which HSV-TK gene is specifically expressed. A 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound is denoted by the chemical formula 1. A method for manufacturing the 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound comprises: a step of reacting anhydrous trifluoro methanesulfonyl in a compound of the chemical formula 2 under the presence of organic solvent to produce the tribenzoyl triflate saccharide compound of the chemical formula 3; a step of introducing fluorine-18 to produce a compound of the chemical formula 4; a step of reacting the compound of the chemical formula 4 with anhydrous acetic acid under the presence of organic solvent to produce a compound of the chemical formula 5; a step of reacting the compound of the chemical formula 5 with silylated thymine to produce a compound of the chemical formula 7; and a step of hydrolyzing the compound of the chemical formula 7 to produce the compound of the chemical formula 1.

Abstract translation: 提供了制备2-脱氧-2- [18 F]氟-5-甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物的制备方法，通过在细胞系中特异性活化以产生高摄入率的化合物，其中HSV-TK 基因被特异表达。 2-脱氧-2- [18 F]氟-5-甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物由化学式1表示。制备2-脱氧-2- [18 F]氟-5- 甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物包括：在有机溶剂的存在下，使化学式2的化合物中的无水三氟甲烷磺酰化反应生成化学式3的三苯甲酰基三氟甲磺酸酯化合物的步骤; 引入氟-18以制备化学式4的化合物的步骤; 在有机溶剂的存在下使化学式4的化合物与无水乙酸反应以产生化学式5的化合物的步骤; 使化学式5的化合物与甲硅烷基化的胸腺嘧啶反应以产生化学式7的化合物的步骤; 以及水解化学式7的化合物以制备化学式1的化合物的步骤。