Synthesis of the bifunctional chelator NHS-SHNH

QIN Guangming  ZHANG Yongxue  AN Rui

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Synthesis of the bifunctional chelator NHS-SHNH

更新时间：2021-03-12

- Synthesis of the bifunctional chelator NHS-SHNH
- NUCLEAR TECHNIQUES Issue 12, (2002)
- 作者机构：
  
  1. 华中科技大学同济医学院附属协和医院核医学科
  2. 华中科技大学同济医学院化学教研室
  4. ,武汉,430030
- 作者简介：
- 基金信息：
- DOI：
  CLC： TQ421
- Published：01 December 2002
- 稿件说明：
移动端阅览
[1]秦光明,张永学,安锐,李桂玲,夏淑贞.双功能螯合剂联肼尼克酰胺衍生物的合成[J].核技术,2002(12):1003-1006.

QIN Guangming ZHANG Yongxue AN Rui. Synthesis of the bifunctional chelator NHS-SHNH[J]. Nuclear techniques, 2002, (12): 1003-1006.
[1]秦光明,张永学,安锐,李桂玲,夏淑贞.双功能螯合剂联肼尼克酰胺衍生物的合成[J].核技术,2002(12):1003-1006. DOI：

QIN Guangming ZHANG Yongxue AN Rui. Synthesis of the bifunctional chelator NHS-SHNH[J]. Nuclear techniques, 2002, (12): 1003-1006. DOI：

摘要

6 -氯尼克酸与水合肼反应生成 6 -联胺吡啶 - 3-羧酸

后者与二叔丁基碳酸酯反应生成6 -BOC -联胺吡啶 - 3-羧酸

使联胺基团得到保护。在DCC、DMF催化下

6 -BOC -联胺吡啶- 3-羧酸与NHS反应

生成物在盐酸二恶烷作用下脱去BOC保护基团

最终生成NHS -SHNH双功能螯合剂

Abstract

Chloronictinic acid reacts with hydrazine hydrate to give 6-hydrazinopiridine-3-carboxylic acid

and the latter then reacts with di-tert-buty dicarbonate to produce 6-BOC-hydrazinopiridin-3-carboxylic acid

which has the hydrazino group protected by BOC. After the NHS is conjugated with 6-BOC-hydrazinopiridin-3-carboxylic acid

the BOC group is eliminated by adding the HCl/dioxane solution to give the final product.

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