[Back]

U. Jordis, J. Fröhlich, M. Treu, M. Hirnschall, L. Czollner, B. Kaelz, S. Welzig:
"Preparation of galanthamine analogs for pharmaceutical use as acetyl- and butyrylcholinesterase inhibitors";
Patent: PCT, No. WO 0174820; submitted: 03-22-2001, granted: 10-11-2001.

Galanthamine derivs. and analogs, such as I [R1, R2 = H, Cn, OH, SH, NO2, SO3H, PO3H, NH2, halogen, etc.; R3 = OH, OMe; R4 = OH, alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, aryloxy, etc.; G1, G2, G3 = CH2, (CH2)2, (CH2)3, CH(OH), etc.; W = CH2, NR5, etc.; R5 = alkyl, acyl, aryl, etc.], were prepd. for therapeutic use as acetyl- and butyrylcholinesterase inhibitors. Thus, ()-galanthamine deriv. II was prepd. in 80.8% yield by condensation of ()-norgalanthamine with 2-chloropyrimidine using NaHCO3 in EtOH. The prepd. galanthamine derivs. and analogs were tested for acetyl- and butyrylcholinesterase inhibiting activity.
AN 2001:747793