1149. Bepotastine

Nomenclature

CAS number: 190786-43-7
4-[(S)-(4-Chlorophenyl)-2-pyridinylmethoxy]-1-piperidinebutanoic acid; betotastine.
C21H25ClN2O3; mol wt 388.89.
C 64.86%, H 6.48%, Cl 9.12%, N 7.20%, O 12.34%.

Description and references

Histamine H1-receptor antagonist. Prepn (stereochem. unspec.): A. Koda et al., EP 335586; eidem, US 4929618 (1989, 1990 both to Ube). Prepn of optically active salts: J. Kita et al., EP 949260 (1999 to Ube; Tanabe Seiyaku). Pharmacology: M. Kato et al., Arzneim.-Forsch. 47, 1116 (1997). Suppression of IL-5 production: O. Kaminuma et al., Biol. Pharm. Bull. 21, 411 (1998). Antiallergic activity in animal models: M. Ueno et al., Pharmacology 57, 206 (1998).

Chemical structure

Derivative

Benzenesulfonate salt.

Nomenclature

CAS number: 190786-44-8
Bepotastine besilate; TAU-284; Talion (Tanabe).
C21H25ClN2O3.C6H6O3S; mol wt 547.06.
C 59.28%, H 5.71%, Cl 6.48%, N 5.12%, O 17.55%, S 5.86%.

Properties

Pale grey prisms from acetonitrile, mp 161-163°. [α]D20 +6.0° (c = 5 in methanol).

Therapeutic Category

Antihistaminic.

Keywords

Antihistaminic