1993. Cerivastatin

Nomenclature

CAS number: 145599-86-6
(3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic acid; (3R,5S,6E)-7-[4-(p-fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)-3-pyridyl]-3,5-dihydroxy-6-heptenoic acid.
C26H34FNO5; mol wt 459.55.
C 67.95%, H 7.46%, F 4.13%, N 3.05%, O 17.41%.

Description and references

HMG-CoA reductase inhibitor. Prepd and claimed as methyl ester: R. Angerbauer et al., EP 325130; eidem, US 5006530; as (+)-form sodium salt: eidem, US 5177080 (1989, 1991, 1993 all to Bayer). Determn in plasma by fluorescence linked LC: G. J. Krol et al., J. Pharm. Biomed. Anal. 11, 1269 (1993); by HPLC: eidem, Methodol. Surv. Bioanal. Drugs 23, 147 (1994). Effects on LDL receptor levels: G. C. Ness et al., Arch. Biochem. Biophys. 325, 242 (1996). Pharmacokinetics in dogs and rats: W. Steinke et al., Jpn. Pharmacol. Ther. 24 Suppl. 9, S1217 (1996). Clinical trial in hyperlipidemia: N. Nakaya et al., ibid. S1381.

Chemical structure

Derivative

Sodium salt.

Nomenclature

CAS number: 143201-11-0
Rivastatin; Bay w 6628; Baycol (Bayer); Lipobay (Bayer).
C26H33FNNaO5; mol wt 481.53.
C 64.85%, H 6.91%, F 3.95%, N 2.91%, Na 4.77%, O 16.61%.

Properties

Solid, [α]D20 +24.1° (c = 1 in ethanol).

Therapeutic Category

Antilipemic.

Keywords

Antilipemic; HMG CoA Reductase Inhibitors; HMG CoA Reductase Inhibitor