9129. Telmisartan

Nomenclature

CAS number: 144701-48-4
4′-[(1,4′-Dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl][1,1′-biphenyl]-2-carboxylic acid; 4′-[[4-methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl]methyl]-2-biphenylcarboxylic acid; BIBR 277; Kinzalmono (Bayer); Micardis (Boehringer, Ing.); Pritor (GSK).
C33H30N4O2; mol wt 514.62.
C 77.02%, H 5.88%, N 10.89%, O 6.22%.

Description and references

Angiotensin II receptor antagonist. Prepn: N. Hauel et al., EP 502314 (1992 to Thomae), C.A. 117, 251352 (1992); U. J. Ries et al., J. Med. Chem. 36, 4040 (1993). Large-scale synthesis: K. S. Reddy et al., Org. Process Res. Dev. 11, 81 (2007). Pharmacology: W. Wienen et al., Br. J. Pharmacol. 110, 245 (1993). Binding study: W. Wienen, M. Entzeroth, J. Hypertens. 12, 119 (1994). Clinical pharmacology, pharmacokinetics: J. M. Neutel, D. H. G. Smith, Adv. Ther. 15, 206 (1998). Clinical trial in hypertension: D. H. G. Smith et al., ibid. 229. Review of pharmacology and clinical efficacy: K. J. McClellan, A. Markham, Drugs 56, 1039-1044 (1998).

Chemical structure

Properties

White solid, mp 261-263°. Practically insol in water (pH 3-9). Sparingly sol in strong acid (except insol in hydrochloric acid); sol in strong base.

Therapeutic Category

Antihypertensive.

Keywords

Angiotensin II Receptor Antagonist; Antihypertensive