Abstract:The preparation, isolation, and melting points of 45 new 4-alkoxy-A,A-dialkyl-l-naphthamidine hydrochlorides with the alkoxy alkyl = Me through C13H» and the A-alkyl = Et through C8Hl7 are outlined. A brief discussion of the limitations of several synthetic routes to sterically hindered amidines is given. Approximate oral LD» values and therapeutic indices (TI) against the cestodes (tapeworms) Hymenolepis nana and Oochoristica symmetrica of these and related -naphthamidines in the mouse are given. A broad band… Show more
“…A large number of 4-alkoxy-l-naphthamidines have been prepared [260,261] in order to establish a structure-activity relationship as also to search for a better compound; however, none were found to exceed the potency of CXXXIV. This study indicated that the optimal cestodicidal activity in 4-alkoxy-l-naphthamidines lies when the total number of carbon atoms ofalkoxy chain and the amidine group is between 12 and 23.…”
“…A large number of 4-alkoxy-l-naphthamidines have been prepared [260,261] in order to establish a structure-activity relationship as also to search for a better compound; however, none were found to exceed the potency of CXXXIV. This study indicated that the optimal cestodicidal activity in 4-alkoxy-l-naphthamidines lies when the total number of carbon atoms ofalkoxy chain and the amidine group is between 12 and 23.…”
Die Alkoxynaphthonitrile (I) lassen sich durch Erhitzen mit den aus den entsprechenden sekundären Aminen (IV) und Äthylmagnesiumbromid darstellbaren Dialkylaminomagnesiumbromiden (II) zu den Amidinen (III) umsetzen.
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