Synthesis and Anticholinesterase Properties of Diacetylene Diamines.-All diacetylene diamines (VI), synthesized by Mannich reaction of α,ω-diacetylenes with amines and formaldehyde, possess non-selective anticholinesterase activity. It is shown, that the biological activity is reduced in sterically strained tertiary amines like N-benzyl derivative (VIc). Introduction of a diphenylpolymethylene bridge [cf. compound (VIb)], however, increases the activity. -(LIBMAN, N. M.; KUZNETSOV, S. G.; ZLOBINA, V. I.; MORALEV, S. N.; KORMILITSYN, B. N.; ANDROSOV, N. S.; Khim.-Farm. Zh. 32 (1998) 9, 20-22; Inst. toksikol. Minzdravmedproma Rossii, St. Petersburg, Russia; RU)
Cyclopentyl‐MgCl (I) reagiert mit dem Benzoesäureester (II) zum Carbinol (III); dieses Carbinol bzw. sein Benzoesäureester entstehen auch bei der Reaktion der Grignard‐Verbindung (I) mit Benzoesäuredimethylamid bzw. Benzoyl‐ Chlorid.
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