Synthesis of ω-[18F]fluoroalkyl analogs of YM-09151-2 for the measurement of D2-dopamine receptors with PET

Kentaro Hatano, Tatsuo Ido, Kiichi Ishiwata, Jun Hatazawa, Masatoshi Itoh, Koichiro Kawashima, Ren Iwata

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)

Abstract

Two [18F]fluoroalkyl analogs of a neuroleptic YM-09151-2 were synthesized via nucleophilic [18F]fluorination of methanesulfonyloxy- or p-toluenesulfonyloxyalkyl derivatives using no-carrier-added [18F]fluoride. Although 3-[18F]fluoropropylaminobenzamide was obtained in good yield, the yield of 2-[18F]fluoroethyl derivative was severalfold lower. The product, N-[(2RS,3RS)-1-benzyl-2-methylpyrrolidin-3-yl]-5-chloro-2-methoxy-4-(3-[ 18F]fluoropropyl)-aminobenzamide, was shown to have a striatum-to-cerebellum ratio comparable to that of 11C labeled YM-09151-2 and thus to be a good candidate for measuring D2-receptors in vivo.

Original languageEnglish
Pages (from-to)551-555
Number of pages5
JournalInternational Journal of Radiation Applications and Instrumentation. Part
Volume41
Issue number6
DOIs
Publication statusPublished - 1990

ASJC Scopus subject areas

  • Radiation
  • Engineering(all)

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