10035. Vorozole

Nomenclature

CAS number: 129731-10-8
6-[(S)-(4-Chlorophenyl)-1H-1,2,4-triazol-1-ylmethyl]-1-methyl-1H-benzotriazole; (+)-(S)-6-[4-chloro-α-(1H-1,2,4-triazol-1-yl)benzyl]-1-methyl-1H-benzotriazole; R-83842; Rivizor (J & J).
C16H13ClN6; mol wt 324.77.
C 59.17%, H 4.03%, Cl 10.92%, N 25.88%.

Description and references

Nonsteroidal aromatase inhibitor. Prepn: A. H. M. Raeymaekers et al., EP 293978 (1988 to Janssen); resolution of enantiomers: A. L. A. Willemsens et al., WO 9411364 (1994 to Janssen). Aromatase inhibition by racemate: W. Wouters et al., J. Steroid Biochem. 32, 781 (1989); and enantiomers: eidem, J. Steroid Biochem. Mol. Biol. 37, 1049 (1990). Abs config: O. M. Peeters et al., Acta Crystallogr. C49, 1958 (1993). Clinical studies in breast cancer: S. R. D. Johnston et al., Cancer Res. 54, 5875 (1994); P. E. Goss et al., Clin. Cancer Res. 1, 287 (1995). Review of clinical pharmacology and pharmacokinetics: W. Wouters et al., Breast Cancer Res. Treat. 30, 89-94 (1994).

Chemical structure

Properties

Crystals from 2-propanol, mp 130-135°. [α]D20 +8.0° (c = 10 in CH3OH).

Derivative

(±)-Form.

Nomenclature

CAS number: 118949-22-7
R-76713.

Properties

Crystals from 2-propanone/1,1-oxybisethane, mp 178.9°.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic (Hormonal); Aromatase Inhibitors; Aromatase Inhibitors