11 C]Hydroxyurea has been successfully labelled using [ 11 C]carbon monoxide at low concentration. The decay-corrected radiochemical yield was 38 AE 3%, and the trapping efficiency of [ 11 C]carbon monoxide in the order of 90 AE 5%. This synthesis was performed by a rhodium-mediated carbonylation
The synthesis and use of [14C]carbon monoxide in Pd-catalyzed carbonylation reactions
β Scribed by Charles S. Elmore
- Publisher
- John Wiley and Sons
- Year
- 2010
- Tongue
- French
- Weight
- 178 KB
- Volume
- 54
- Category
- Article
- ISSN
- 0022-2135
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β¦ Synopsis
Abstract
The [^14^C]carbonylation reaction is a very powerful method of incorporating Cβ14 into a drug molecule late in a radiochemical synthesis. The first and perhaps most critical step in [^14^C]carbonylation reactions is the generation of ^14^CO and its subsequent delivery to the reaction flask. There are three published methods for generating ^14^CO: conversion of ^14^CO~2~ with Zn at 400Β°C, pyrolysis of Ca^14^CO~3,~ and dehydration of NaOCH. Additionally, a newly published method for the in situ carbonylation of aryl and vinyl halides to give acids has been investigated using NaOCH as the labeled precursor. Finally, the application of ^14^CO in Pdβcatalyzed [^14^C]carbonylation reactions will be discussed. Copyright Β© 2010 John Wiley & Sons, Ltd.
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