N. V. Smirnova

Curare-like action of monoquaternary salts containing an adamantyl group on the nitrogen atom

In activity cer ta in of these compounds may compare with the most effective muscle relaxants which belong to the group of b isquaternary ammonium salts. Like the major i ty of monoquaternary salts their ac tion is quite shortl ived. This is evidently associated to a considerable degree with the p resence of hydrolyzable es te r bonds in the organism. The disadvantages of compounds of the types (I) and (II) which hinder their use in anesthetic prac t ice must be attributed to the fact that they cause a depolarized neuromuscular block. As is known, antidepotarizing muscle relaxants are of most interest for surgical use [2] and the a c tion of these must be regulated by the use of antagonists (for example neostigmine). Fur the rmore , they do not disturb the distribution of the potass ium ions and in this connection do not lead to the onset of a ser ies of side effects which are charac te r i s t i c of depolarizing compounds.

SYNTHESIS AND PHARMACOLOGICAL PROPERTIES OF THE DIIODOMETHYLATE OF BIS‐(BETA‐(N‐METHYL‐N‐1‐ADAMANTYL)AMINOETHYL) ESTER OF SUCCINIC ACID (DIADONIUM)

Bernsteinsauremethylester (I) reagiert mit β-(N-Methyl-N-(l-adamantyl)amino)- athanol (II) in Gegenwart von Natrium unter Stickstoff bei 100°C in 6l%iger Ausbeute zum Ester (III), dessen Umsetzung mit Methyljodid in Aceton in 80%iger Ausbeute zum Bisquartarsalz (IV) (Diadonium) fuhrt, das eine starke, nicht lange anhaltende Curare-ahnliche Wirksamkeit besitzt.