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

✍ Scribed by Kentaro Hatano; Tatsuo Ido; Kiichi Ishiwata; Jun Hatazawa; Masatoshi Itoh; Koichiro Kawashima; Ren Iwata

Publisher
Elsevier Science
Year
1990
Weight
476 KB
Volume
41
Category
Article
ISSN
0883-2889

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✦ Synopsis

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.

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