Development of fluorine-18-labeled 5-HT1A antagonists

L Lang, E Jagoda, B Schmall, BK Vuong…

Index: Lang, Lixin; Jagoda, Elaine; Schmall, Bernard; Vuong, Bik-Kee; Adams, H. Richard; Nelson, David L.; Carson, Richard E.; Eckelman, William C. Journal of Medicinal Chemistry, 1999 , vol. 42, # 9 p. 1576 - 1586

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Citation Number: 111

Abstract

We have synthesized five fluorinated derivatives of WAY 100635, N-{2-[4-(2-methoxyphenyl) piperazino] ethyl}-N-(2-pyridyl) cyclohexanecarboxamide (4a), using various acids in place of the cyclohexanecarboxylic acid (CHCA, 2a) in the reaction scheme. The five acids are 4- fluorobenzoic acid (FB, 2b), 4-fluoro-3-methylbenzoic acid (MeFB, 2c), trans-4- fluorocyclohexanecarboxylic acid (FC, 2d), 4-(fluoromethyl) benzoic acid (FMeB, 2e), and ...