| 摘要 |
The invention comprises 9-substituted 1 : 10-diaza-anthracenes (1-aza-acridines) having, in one tautomeric form, the general formula <FORM:0769023/IV(b)/1> (wherein R represents an alkoxy group of 1-6 carbon atoms, Y represents hydrogen or a halogen (preferably in the 6-position), R1 represents a mono- or di-hydroxyalkyl group of 2-6 carbon atoms, and n is an integer from 2 to 6) and their acid addition salts, and the preparation of the free bases or their hydrohalides by heating the corresponding compound substituted in the 9-position by a halogen atom or a phenoxy or alkyl- or polyalkyl-substituted phenoxy group, with a hydroxyamine H2N.(CH2)n.NHR1, advantageously in the presence of an inert solvent. The 9-phenoxy compounds may be prepared, if desired in situ, by heating the 9-halo compounds with phenol, a cresol, a xylenol or other polyalkylphenol, or mixtures thereof, which may be used in excess to provide a solvent for the reaction with the amine. The products of the latter reaction are useful as anthelmintics. Examples describe the interaction of 2-methoxy-6 : 9 - dichloro - 1 : 10 - diaza - anthracene with 2 - (21 : 31 - dihydroxy - n - propylamino) - ethylamine, 2 - (21 - hydroxypropylamino) - ethylamine, 2 - (21 - hydroxyethylamino) - ethylamine and 3-(21 : 31-dihydroxypropylamino)-ethylamine, of 2 - n - butoxy - 6 : 9-dichloro-1 : 10 - diazo - anthracene with 2 -(21 - hydroxypropylamino)-ethylamine, and of 2-methoxy-9-chloro - 1 : 10 - diaza - anthracene with 2 - (21 - hydroxyethylamino) - ethylamine. Additional reactants are listed. Starting material. 2 - (21 : 31 - Dihydroxy - n - propylamino)-ethylamine is obtainable by reacting ethylene diamine with glycerol a -monochlorhydrin. Specification 704,238 is referred to. |
