| 摘要 |
<p>4-(Bis(4-fluoro phenyl) methylene)piperidine derivs. are made by (a) treatment of 4-fluoro-benzoyl piperidine with 4-fluoro-phenyl magnesium bromide; (b) dehydrating the prod to obtain 4-(bis(4-fluorophenyl)methylene)piperidine; (c) reacting this with 2-(omega-halo alkyl derivs. of ethyl aceto-acetate, e.g. ethyl 4-bromo 2-acetyl butyrate or ethyl 5-bromo 2-acetyl pentanoate, in toluene, xylene or dioxane; and (c) treating the prod. with 2-amino pyridine, 2-amino 4-chloro pyridine or 2-amino 4-methoxy pyridine, in presence of POCl3 and polyphosphoric acid, to obtain derivs. of 2-methyl 3-(2-(4-bis (4-fluorophenyl) methylene)1-piperidinyl) ethyl)4H-pyrido (1,2-a) pyrimidin-4-one and its acceptable acid addn. salts.</p> |
