Radical fluoroarylation in radiochemical synthesis

Christina Hultsch; Olga Blank; Hans Jürgen Wester; Markus R. Heinrich

doi:10.1016/j.tetlet.2007.12.128

Radical fluoroarylation in radiochemical synthesis

Christina Hultsch, Olga Blank, Hans Jürgen Wester, Markus R. Heinrich

Chair of Pharmaceutical Radiochemistry

Technical University of Munich

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

In this study, we report on the radical [¹⁸F]fluoroarylation of different olefins using 4-[¹⁸F]fluorobenzenediazonium ions to provide a new route to radiopharmaceuticals containing a deactivated, 4-[¹⁸F]fluoro substituted phenyl group. This new methodology was shown to be well suited for the synthesis of ¹⁸F-labelled stilbenes. Stilbene 7 is now accessible within 80 min in 30-45% overall radiochemical yield starting from [¹⁸F]fluoride.

Original language	English
Pages (from-to)	1881-1883
Number of pages	3
Journal	Tetrahedron Letters
Volume	49
Issue number	11
DOIs	https://doi.org/10.1016/j.tetlet.2007.12.128
State	Published - 10 Mar 2008

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10.1016/j.tetlet.2007.12.128

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title = "Radical fluoroarylation in radiochemical synthesis",

abstract = "In this study, we report on the radical [18F]fluoroarylation of different olefins using 4-[18F]fluorobenzenediazonium ions to provide a new route to radiopharmaceuticals containing a deactivated, 4-[18F]fluoro substituted phenyl group. This new methodology was shown to be well suited for the synthesis of 18F-labelled stilbenes. Stilbene 7 is now accessible within 80 min in 30-45\% overall radiochemical yield starting from [18F]fluoride.",

author = "Christina Hultsch and Olga Blank and Wester, \{Hans J{\"u}rgen\} and Heinrich, \{Markus R.\}",

note = "Funding Information: This project was financed by the Fonds der Chemischen Industrie (Liebig fellowship). We are grateful to the Leonhard-Lorenz-Stiftung of the Technische Universit{\"a}t M{\"u}nchen. The generous help and support of Professor Dr. Thorsten Bach and his group is gratefully acknowledged. ",

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doi = "10.1016/j.tetlet.2007.12.128",

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journal = "Tetrahedron Letters",

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T1 - Radical fluoroarylation in radiochemical synthesis

AU - Hultsch, Christina

AU - Blank, Olga

AU - Wester, Hans Jürgen

AU - Heinrich, Markus R.

N1 - Funding Information: This project was financed by the Fonds der Chemischen Industrie (Liebig fellowship). We are grateful to the Leonhard-Lorenz-Stiftung of the Technische Universität München. The generous help and support of Professor Dr. Thorsten Bach and his group is gratefully acknowledged.

PY - 2008/3/10

Y1 - 2008/3/10

N2 - In this study, we report on the radical [18F]fluoroarylation of different olefins using 4-[18F]fluorobenzenediazonium ions to provide a new route to radiopharmaceuticals containing a deactivated, 4-[18F]fluoro substituted phenyl group. This new methodology was shown to be well suited for the synthesis of 18F-labelled stilbenes. Stilbene 7 is now accessible within 80 min in 30-45% overall radiochemical yield starting from [18F]fluoride.

AB - In this study, we report on the radical [18F]fluoroarylation of different olefins using 4-[18F]fluorobenzenediazonium ions to provide a new route to radiopharmaceuticals containing a deactivated, 4-[18F]fluoro substituted phenyl group. This new methodology was shown to be well suited for the synthesis of 18F-labelled stilbenes. Stilbene 7 is now accessible within 80 min in 30-45% overall radiochemical yield starting from [18F]fluoride.

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U2 - 10.1016/j.tetlet.2007.12.128

DO - 10.1016/j.tetlet.2007.12.128

M3 - Article

AN - SCOPUS:38949151586

SN - 0040-4039

VL - 49

SP - 1881

EP - 1883

JO - Tetrahedron Letters

JF - Tetrahedron Letters

IS - 11

ER -

Radical fluoroarylation in radiochemical synthesis

Abstract

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