[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

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

12 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",

month = jan,

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

language = "English",

volume = "49",

pages = "73--77",

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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