一锅法自动化合成3’-脱氧-3’-<sup>18</sup>F-氟代胸苷和O-(2-<sup>18</sup>F-氟代乙基)-L-酪氨酸

唐刚华; 唐小兰; 王明芳; 李葆元; 梁明泉

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一锅法自动化合成3’-脱氧-3’-¹⁸F-氟代胸苷和O-(2-¹⁸F-氟代乙基)-L-酪氨酸

核化学、放射性药物和核医学 | 更新时间：2021-03-12

- 一锅法自动化合成3’-脱氧-3’-¹⁸F-氟代胸苷和O-(2-¹⁸F-氟代乙基)-L-酪氨酸
- Automated synthesis of 3’-deoxy-3’-[¹⁸F]fluorothymidine and O-(2-¹⁸F-fluoroethyl)-L-tyrosine as tumor imaging agents
- 核技术 2009年32卷第2期
- 作者机构：
  
  1. 南方医科大学南方医院核医学科PET中心
  2. 中山大学附属第一医院核医学科PET-CT中心
  3. 华南农业大学理学院
- 作者简介：
- 基金信息：
  
  (No.ZX069);(No.ZX069)
- DOI：
  中图分类号： R817.9
- 纸质出版日期：2009-02-01
- 稿件说明：
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[1]唐刚华,唐小兰,王明芳,李葆元,梁明泉.一锅法自动化合成3’-脱氧-3’-~(18)F-氟代胸苷和O-(2-~(18)F-氟代乙基)-L-酪氨酸[J].核技术,2009,32(02):154-160.

TANG Ganghua1, 3 TANG Xiaolan2 WANG Mingfang1 LI Baoyuan1 LIANG Mingquan1 1. Automated synthesis of 3’-deoxy-3’-[¹⁸F]fluorothymidine and O-(2-¹⁸F-fluoroethyl)-L-tyrosine as tumor imaging agents[J]. Nuclear techniques, 2009, 32(2): 154-160.
[1]唐刚华,唐小兰,王明芳,李葆元,梁明泉.一锅法自动化合成3’-脱氧-3’-~(18)F-氟代胸苷和O-(2-~(18)F-氟代乙基)-L-酪氨酸[J].核技术,2009,32(02):154-160. DOI：

TANG Ganghua1, 3 TANG Xiaolan2 WANG Mingfang1 LI Baoyuan1 LIANG Mingquan1 1. Automated synthesis of 3’-deoxy-3’-[¹⁸F]fluorothymidine and O-(2-¹⁸F-fluoroethyl)-L-tyrosine as tumor imaging agents[J]. Nuclear techniques, 2009, 32(2): 154-160. DOI：

摘要

采用"一锅法"和TRACERlab FXF-N自动化合成装置

以3-N-t-叔丁氧羰基-1-[5’-O-（4

4’-二甲氧基三苯甲基）-2’-脱氧-3’-O-（4-硝基苯磺酰基）-β-D-苏型阿呋喃糖基]胸腺嘧啶为前体

在同一反应瓶中经亲核氟化、盐酸水解两步反应及HPLC分离纯化制备18F-FLT注射液。以乙二醇二对甲苯磺酸酯为起始原料

在同一反应瓶中经亲核氟化和烷基化两步反应及HPLC分离纯化得18F-FET注射液。18F-FLT和18F-FET总合成时间分别约为60min和50min

未校正的放化产率均大于20%

放化纯度均大于95%。18F-FLT和18F-FET注射液质量控制指标符合放射性药物质量要求。

Abstract

For early diagnosis for malignant tumors with the different metabolic imaging agents

a fully automated synthetic technology of 3’-deoxy-3’-[18F]fluorothymidine (18F-FLT) and O-(2-18F-fluoroethyl)-L-tyrosine (18F-FET) was studied in this paper. Automated synthesis of 18F-FLT and 18F-FET was performed by one-pot two-step reaction procedure at TRACERlab FXF-N system. 18F-FLT injection was obtained via two-step reaction including nucleophilic fluorination of 3-N-t-butoxycarbonyl-1-[5’-O-(4

4’-di-methoxytriphenylmethyl)-2’-deoxy-3’-O-(4-nitrobenzenesulfonyl)- β-D-threopentofuranosyl]thymine

the precursor molecule

with 18F-fluoride and subsequent hydrolysis of the pro- tecting group with 1 mol/L HCl at the same reaction vessel

and purification with HPLC system. 18F-FET injection was also prepared via two-step reaction including nucleophilic fluorination of 1

2-di(4-methylphenylsulfonyloxy)ethane as the starting material and following by alkylation of L-tyrosine at the same reaction vessel

and purification with HPLC system. Fully automated synthesis of 18F-FLT and 18F-FET was completed within the total synthesis time of about 50 and 60 min

respectively. The uncorrected radiochemical yields of 18F-FLT and 18F-FET were above 20% and radiochemical purities were more than 95%. The quality control indexes of 18F-FLT and 18F-FET injection meet the requirements of radiopharmaceuticals quality.

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一锅法自动化合成3’-脱氧-3’-18F-氟代胸苷和O-(2-18F-氟代乙基)-L-酪氨酸

Automated synthesis of 3’-deoxy-3’-[18F]fluorothymidine and O-(2-18F-fluoroethyl)-L-tyrosine as tumor imaging agents

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摘要

Abstract

关键词

Keywords

references

一锅法自动化合成3’-脱氧-3’-¹⁸F-氟代胸苷和O-(2-¹⁸F-氟代乙基)-L-酪氨酸

Automated synthesis of 3’-deoxy-3’-[¹⁸F]fluorothymidine and O-(2-¹⁸F-fluoroethyl)-L-tyrosine as tumor imaging agents