| 摘要 |
<p>Cpds. of formula (where R = p-halo- or p-alkoxy-phenyl, or heterocyclic preferably thienyl) are useful as anti-histamines and spasmolytics, and have CNS activity. This can be used to treat pruriginous dermatosis, allergic respiratory disorders, neuropsychiatric disorders such as over-excitement and digestive disorders. They are prepd. in four steps. (i) 1-(p-chlorophenyl)-piperazine + trioxymethylene in acetone gives 1-(p-chlorophenyl)-4-(3-oxobutyl)-piperazine. (ii) This is converted to its oxime with NH2OH. (iii) This is reduced to the 3-aminobutyl compound with H2+Raney Ni. (iv) This amine is treated with R-CO-Cl. The prefd. dose is 2.5-40 mg. depending on the administration type.</p> |
