Synthesis of 11C-Labelled Symmetrical Ureas via the Rapid Incorporation of [11C]CO2 into Aliphatic and Aromatic Amines

被引：20

作者：

Dheere, Abdul Karim Haji ^{[1
]}

Bongarzone, Salvatore ^{[1
]}

Taddei, Carlotta ^{[1
]}

Yan, Ran ^{[1
]}

Gee, Antony D. ^{[1
]}

机构：

[1] Kings Coll London, Div Imaging Sci & Biomed Engn, London SE1 7EH, England

来源：

SYNLETT | 2015年 / 26卷 / 16期

基金：

英国工程与自然科学研究理事会; 英国医学研究理事会;

关键词：

carbon-11; carbon dioxide; Mitsunobu reaction; symmetrical urea; DBU; CARBONYLATION REACTIONS; ONE-POT; C-11; PET; CARBOXYLATION; DERIVATIVES; MITSUNOBU; FIXATION; CO2;

D O I：

10.1055/s-0034-1381055

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient method to radiolabel symmetrical [C-11] ureas using 1,8-diazabicycloundec-7-ene (DBU) and cyclotron-produced [C-11]CO2 has been developed. [C-11] urea derivatives were obtained when aliphatic and aromatic amines were used with excellent radiochemical yields (RCYs) of over 70%. The mechanism of the reaction is proposed on the basis of control experiments. This simple and robust methodology provides a powerful tool to prepare C-11-labelled ureas previously inaccessible by existing methods and enable their utilisation for in vivo molecular imaging applications.

引用

页码：2257 / 2260

页数：4

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