Title: Vorozole
CAS Registry Number: 129731-10-8
CAS Name: 6-[(S)-(4-Chlorophenyl)-1H-1,2,4-triazol-1-ylmethyl]-1-methyl-1H-benzotriazole
Additional Names: (+)-(S)-6-[4-chloro-a-(1H-1,2,4-triazol-1-yl)benzyl]-1-methyl-1H-benzotriazole
Manufacturers' Codes: R-83842
Trademarks: Rivizor (J & J)
Molecular Formula: C16H13ClN6
Molecular Weight: 324.77
Percent Composition: C 59.17%, H 4.03%, Cl 10.92%, N 25.88%
Literature 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).
Properties: Crystals from 2-propanol, mp 130-135°. [a]D20 +8.0° (c = 10 in CH3OH).
Melting point: mp 130-135°
Optical Rotation: [a]D20 +8.0° (c = 10 in CH3OH)
Derivative Type: (±)-Form
CAS Registry Number: 118949-22-7
Manufacturers' Codes: R-76713
Properties: Crystals from 2-propanone/1,1-oxybisethane, mp 178.9°.
Melting point: mp 178.9°
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic (Hormonal); Aromatase Inhibitors; Aromatase Inhibitors. |