8240. Rivastigmine

Nomenclature

CAS number: 123441-03-2
Ethylmethylcarbamic acid 3-[(1S)-1-(dimethylamino)ethyl]phenyl ester; (S)-N-ethyl-3-[(1-dimethylamino)ethyl]-N-methylphenylcarbamate.
C14H22N2O2; mol wt 250.34.
C 67.17%, H 8.86%, N 11.19%, O 12.78%.

Description and references

Brain selective acetylcholinesterase inhibitor. Prepn: A. Enz, DE 3805744; idem, US 5602176 (1988, 1997 both to Sandoz); and activity: R. Amstutz et al., Helv. Chim. Acta 73, 739 (1990). Pharmacology: A. Enz et al., Prog. Brain Res. 98, 431 (1993). Clinical trial in Alzheimer's disease: M. R"osler et al., Br. Med. J. 318, 633 (1999).

Chemical structure

Properties

[α]D20 -32.1° (c = 5 in ethanol).

Derivative

Hydrogen tartrate.

Nomenclature

CAS number: 129101-54-8
ENA-713; SDZ-ENA-713; SDZ-212-713; Exelon (Novartis).
C14H22N2O2.C4H6O6; mol wt 400.42.
C 53.99%, H 7.05%, N 7.00%, O 31.97%.

Properties

Crystals from ethanol, mp 123-125°. [α]D20 +4.7° (c = 5 in ethanol).

Therapeutic Category

Nootropic.

Keywords

Cholinesterase Inhibitor; Nootropic