Synthesis and biological characterization of. alpha.-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogs as potential atypical antipsychotic …

…, WG Lobeck, P Dextraze, E Bernstein…

Index: Yevich, Joseph P.; New, James S.; Lobeck, Walter G.; Dextraze, Pierre; Brenstein, Edith; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 24 p. 4516 - 4525

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Citation Number: 38

Abstract

Method C: RMgX, THF, reflux Method D: CF3COzH, room temp. which was prepared by literature methods from 5-fluorouracil, withN-(ethoxycarbony1) piperazine in acetonitrile afforded 6a. The latter was converted to 5-F-1-PP (8a) by Raney nickel desulfurization followed by acid hydrolysis of the carbamate moiety. Hydrolysis of 6a gave 6b. The 5-chloro (8b) and 5-bromo (&) intermediates were prepared by halogenation of 1-PP or an N- ...