[18F]fluoromethylbenzylsulfonate ester: A rapid and efficient synthetic method for the N[18F]fuoromethylbenzylation of amides and amines

Yearn Seong Choe; Dong Hyuck Song; Kee Jung Lee; Sang Eun Kim; Yong Choi; Kyung Han Lee; Byung Tae Kim; Seung Jun Oh; Dae Yoon Chi

doi:10.1016/S0969-8043(97)00224-8

[¹⁸F]fluoromethylbenzylsulfonate ester: A rapid and efficient synthetic method for the N[¹⁸F]fuoromethylbenzylation of amides and amines

Yearn Seong Choe
, Dong Hyuck Song
, Kee Jung Lee
, Sang Eun Kim
, Yong Choi
, Kyung Han Lee
, Byung Tae Kim
, Seung Jun Oh
, Dae Yoon Chi

Department of Nuclear Medicine

Hanyang University
Inha University

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

13 Scopus citations

Abstract

We have prepared 4-[¹⁸F]fluoromethylbenzylsulfonate esters as fluoromethylbenzylating agents. These agents are readily prepared by an [¹⁸F]fluoride ion displacement of the corresponding bissulfonate esters. The application of these 4-[¹⁸F]fluoromethylbenzylsulfonate esters to N- alkylation reaction of spiperone and 1-phenylpiperazine shows that the products 3-N-(4-[¹⁸F]fluoromethylbenzyl)spiperone and 1-N-(4- [¹⁸F]fluoromethylbenzyl)-4-phenylpiperazine are rapidly produced with high radiochemical yields under a no-carrier-added condition.

Original language	English
Pages (from-to)	73-77
Number of pages	5
Journal	Applied Radiation and Isotopes
Volume	49
Issue number	1-2
DOIs	https://doi.org/10.1016/S0969-8043(97)00224-8
State	Published - Jan 1998

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10.1016/S0969-8043(97)00224-8

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title = "[18F]fluoromethylbenzylsulfonate ester: A rapid and efficient synthetic method for the N[18F]fuoromethylbenzylation of amides and amines",

abstract = "We have prepared 4-[18F]fluoromethylbenzylsulfonate esters as fluoromethylbenzylating agents. These agents are readily prepared by an [18F]fluoride ion displacement of the corresponding bissulfonate esters. The application of these 4-[18F]fluoromethylbenzylsulfonate esters to N- alkylation reaction of spiperone and 1-phenylpiperazine shows that the products 3-N-(4-[18F]fluoromethylbenzyl)spiperone and 1-N-(4- [18F]fluoromethylbenzyl)-4-phenylpiperazine are rapidly produced with high radiochemical yields under a no-carrier-added condition.",

author = "Choe, \{Yearn Seong\} and Song, \{Dong Hyuck\} and Lee, \{Kee Jung\} and Kim, \{Sang Eun\} and Yong Choi and Lee, \{Kyung Han\} and Kim, \{Byung Tae\} and Oh, \{Seung Jun\} and Chi, \{Dae Yoon\}",

year = "1998",

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doi = "10.1016/S0969-8043(97)00224-8",

language = "English",

volume = "49",

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journal = "Applied Radiation and Isotopes",

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TY - JOUR

T1 - [18F]fluoromethylbenzylsulfonate ester

T2 - A rapid and efficient synthetic method for the N[18F]fuoromethylbenzylation of amides and amines

AU - Choe, Yearn Seong

AU - Song, Dong Hyuck

AU - Lee, Kee Jung

AU - Kim, Sang Eun

AU - Choi, Yong

AU - Lee, Kyung Han

AU - Kim, Byung Tae

AU - Oh, Seung Jun

AU - Chi, Dae Yoon

PY - 1998/1

Y1 - 1998/1

N2 - We have prepared 4-[18F]fluoromethylbenzylsulfonate esters as fluoromethylbenzylating agents. These agents are readily prepared by an [18F]fluoride ion displacement of the corresponding bissulfonate esters. The application of these 4-[18F]fluoromethylbenzylsulfonate esters to N- alkylation reaction of spiperone and 1-phenylpiperazine shows that the products 3-N-(4-[18F]fluoromethylbenzyl)spiperone and 1-N-(4- [18F]fluoromethylbenzyl)-4-phenylpiperazine are rapidly produced with high radiochemical yields under a no-carrier-added condition.

AB - We have prepared 4-[18F]fluoromethylbenzylsulfonate esters as fluoromethylbenzylating agents. These agents are readily prepared by an [18F]fluoride ion displacement of the corresponding bissulfonate esters. The application of these 4-[18F]fluoromethylbenzylsulfonate esters to N- alkylation reaction of spiperone and 1-phenylpiperazine shows that the products 3-N-(4-[18F]fluoromethylbenzyl)spiperone and 1-N-(4- [18F]fluoromethylbenzyl)-4-phenylpiperazine are rapidly produced with high radiochemical yields under a no-carrier-added condition.

UR - https://www.scopus.com/pages/publications/0031951509

U2 - 10.1016/S0969-8043(97)00224-8

DO - 10.1016/S0969-8043(97)00224-8

M3 - Article

C2 - 9467837

AN - SCOPUS:0031951509

SN - 0969-8043

VL - 49

SP - 73

EP - 77

JO - Applied Radiation and Isotopes

JF - Applied Radiation and Isotopes

IS - 1-2

ER -

[¹⁸F]fluoromethylbenzylsulfonate ester: A rapid and efficient synthetic method for the N[¹⁸F]fuoromethylbenzylation of amides and amines

Abstract

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