Pd₂(dba)₃/P(MeNCH₂CH₂)₃N路HCl-mediated Stille cross-coupling of [1-¹¹C]acetyl chloride with aryl and heteroaryl stannanes

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• 作者：Takuya Arai ; ^{arai_t@hotmail.co.jp}
• 关键词：Positron emission tomography ; Carbon-11-labeling ; [Carbonyl-11C]acyl chlorides ; Stille cross-coupling reaction
• 刊名：Nuclear Medicine and Biology
• 出版年：2012
• 期刊代码：43_09698051
• 类别：ph
• 出版时间：July, 2012
• 卷：39
• 期：5
• 页码：702-708
• 文件大小：468 K

摘要

Introduction

Developments in the Stille cross-coupling of [1-¹¹C]acetyl chloride with tributylphenylstannane mediated by the Pd₂(dba)₃/P(MeNCH₂CH₂)₃N路HClsystem are reported.

Methods

The reaction conditions for the cross-coupling of [1-¹¹C]acetyl chloride with tributylphenylstannane were optimized, and the reaction scope was investigated.

Results

The cross-couplings of [1-¹¹C]acetyl chloride with a range of aryl and heteroaryl stannanes were performed with good to excellent radiochemical conversions using the developed method.

Conclusions

A highly efficient method for the Stille cross-coupling of [1-¹¹C]acetyl chloride with organostannanes was demonstrated. It is anticipated that our method will be an attractive addition to the carbon-11-labeling procedures available for the synthesis of positron emission tomography probes.