Efficient system for the preparation of [13N]labeled nitrosamines

Vanessa Gómez-Vallejo; Koichi Kato; Masayuki Hanyu; Katsuyuki Minegishi; José I. Borrell; Jordi Llop

doi:10.1016/j.bmcl.2009.02.066

Efficient system for the preparation of [¹³N]labeled nitrosamines

Vanessa Gómez-Vallejo, Koichi Kato, Masayuki Hanyu, Katsuyuki Minegishi, José I. Borrell, Jordi Llop

Producción científica: Artículo en revista indizada › Artículo › revisión exhaustiva

13 Citas (Scopus)

Resumen

In the present Letter, a fast and reproducible method for the synthesis of N-[¹³N]nitrosamines is reported. The labeling strategy is based on trapping [¹³N]NO₂^- in an anion exchange resin. The reaction with secondary amines in the presence of Ph₃P and Br₂ led to the formation of the desired nitrosamines in short reaction times (2 min) with excellent radiochemical conversion (>45%). Final radiotracers were obtained after purification in good radiochemical yields (>30%, decay corrected). Radiochemical purity was above 99% in all cases.

Idioma original	Inglés
Páginas (desde-hasta)	1913-1915
Número de páginas	3
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	19
N.º	7
DOI	https://doi.org/10.1016/j.bmcl.2009.02.066
Estado	Publicada - 1 abr 2009

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title = "Efficient system for the preparation of [13N]labeled nitrosamines",

abstract = "In the present Letter, a fast and reproducible method for the synthesis of N-[13N]nitrosamines is reported. The labeling strategy is based on trapping [13N]NO2- in an anion exchange resin. The reaction with secondary amines in the presence of Ph3P and Br2 led to the formation of the desired nitrosamines in short reaction times (2 min) with excellent radiochemical conversion (>45%). Final radiotracers were obtained after purification in good radiochemical yields (>30%, decay corrected). Radiochemical purity was above 99% in all cases.",

keywords = "Nitrogen-13, Nitrosamines, Positron emission tomography",

author = "Vanessa G{\'o}mez-Vallejo and Koichi Kato and Masayuki Hanyu and Katsuyuki Minegishi and Borrell, {Jos{\'e} I.} and Jordi Llop",

note = "Funding Information: The authors would like to thank Dr. Fujiko Konno, the staff of cyclotron section and personnel of the department of molecular probes of National Institute of Radiological Sciences for helping throughout experimental work. We also thank the Departamento de Industria, Comercio y Turismo of the Vasc Government for financial support.",

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AU - Kato, Koichi

AU - Hanyu, Masayuki

AU - Minegishi, Katsuyuki

AU - Borrell, José I.

AU - Llop, Jordi

N1 - Funding Information: The authors would like to thank Dr. Fujiko Konno, the staff of cyclotron section and personnel of the department of molecular probes of National Institute of Radiological Sciences for helping throughout experimental work. We also thank the Departamento de Industria, Comercio y Turismo of the Vasc Government for financial support.

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N2 - In the present Letter, a fast and reproducible method for the synthesis of N-[13N]nitrosamines is reported. The labeling strategy is based on trapping [13N]NO2- in an anion exchange resin. The reaction with secondary amines in the presence of Ph3P and Br2 led to the formation of the desired nitrosamines in short reaction times (2 min) with excellent radiochemical conversion (>45%). Final radiotracers were obtained after purification in good radiochemical yields (>30%, decay corrected). Radiochemical purity was above 99% in all cases.

AB - In the present Letter, a fast and reproducible method for the synthesis of N-[13N]nitrosamines is reported. The labeling strategy is based on trapping [13N]NO2- in an anion exchange resin. The reaction with secondary amines in the presence of Ph3P and Br2 led to the formation of the desired nitrosamines in short reaction times (2 min) with excellent radiochemical conversion (>45%). Final radiotracers were obtained after purification in good radiochemical yields (>30%, decay corrected). Radiochemical purity was above 99% in all cases.

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