| 摘要 |
<p>Novel guanidine derivatives of the general formula <FORM:1063749/C2/1> (wherein A represents -CH2- or -CH2CH2- and X represents -O-, -S-, -NH-, -NMe- or -NEt-), and their salts with inorganic and organic acids, are prepared by reacting an amine of the general formula <FORM:1063749/C2/2> with a compound of the general formula <FORM:1063749/C2/3> (wherein Y represents a radical that can be split off) or with an acid addition salt thereof, or reacting said amine or an acid addition salt thereof with cyanamide, or by reacting a compound of the general formula <FORM:1063749/C2/4> or an acid addition salt thereof, with ammonia, or reacting a compound of the general formula <FORM:1063749/C2/5> with ammonia or an ammonium salt, or by reacting a reactive ester of a compound of the general formula <FORM:1063749/C2/6> with granidine or with an acid addition salt thereof, and in all cases, if desired, converting a resulting acid addition salt into the free base or vice versa. Alternative methods of preparation are also mentioned. The preparation of the following starting materials is described: adamant-1-yloxyacetamide, b - (adamant - 1 - yloxy) - ethylamine, adamant - 1 - ylthioacetamide, b - (adamant - 1 - ylthio) - ethylamine, b - (adamant - 1 - ylthio)-propionic acid, chloroacetic and azidoacetic acid N-(1-adamantyl)- and N-(1-homoadamantyl)-amides, N - (1 - adamantyl)- and N-(1-homoadamantyl) - ethylenediamine. Pharmaceutical compositions in forms suitable for oral, rectal or parenteral administration as sympathicolytic or antiviral agents comprise at least one compound (I) or acid addition salt thereof and at least one inert carrier.</p> |
