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A combined loop-SPE method for the automated preparation of [11C]doxepin

✍ Scribed by R. Iwata; C. Pascali; A. Bogni; K. Yanai; M. Kato; T. Ido; K. Ishiwata

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
138 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A simple and versatile loop‐solid phase extraction (SPE) method was developed for the automated preparation of [^11^C]doxepin, a histamine H~1~ receptor antagonist, from [^11^C]methyl triflate ([^11^C]MeOTf). This labeling agent was passed through a Teflon or Tefzel loop coated internally with a film of the precursor solution. The reaction products were then flushed from the loop to a short SPE column, where they were concentrated and then injected onto a semi‐preparative HPLC column simply by switching an injection valve. By applying this combined loop‐SPE technique the whole procedure turned out to be easily automated. The formation of [^11^C]methylated doxepin ([^11^C]methyldoxepin) was observed and the ratio of doxepin to methyldoxepin was found to be clearly correlated with the mass ratio of nordoxepin to MeOTf. This observation highlights the importance of [^11^C]MeOTf specific activity in the [^11^C]methylation of secondary amines. Using this method, [^11^C]Doxepin was prepared in over 40% radiochemical yield from high specific activity [^11^C]MeOTf. Copyright © 2002 John Wiley & Sons, Ltd.

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