Title: Fadrozole
CAS Registry Number: 102676-47-1
CAS Name: 4-(5,6,7,8-Tetrahydroimidazo[1,5-
a]pyridin-5-yl)benzonitrile
Synonyms: 5-
p-cyanophenyl-5,6,7,8-tetrahydroimidazo[1,5-
a]pyridine
Molecular Formula: C14H13N3
Molecular Weight: 223.27
Percent Composition: C 75.31%, H 5.87%, N 18.82%
Literature References: Aromatase inhibitor. Prepn: L. J. Browne,
EP 165904;
idem, US 4617307 (1985, 1986 both to Ciba-Geigy); L. J. Browne
et al., J. Med. Chem. 34, 725 (1991). Effects on estrogen biosynthesis: R. E. Steele
et al., Steroids 50, 147 (1987). Pharmacology: K. Schieweck
et al., Cancer Res. 48, 834 (1988). GC/MS determn in plasma and urine: R. Ackermann, G. Kaiser,
Biomed. Environ. Mass Spectrom. 18, 558 (1989). Pharmacokinetics: G. M. Kochak
et al., J. Clin. Endocrinol. Metab. 71, 1349 (1990). Clinical evaluation in metastatic breast cancer: J. I. Raats
et al., J. Clin. Oncol. 10, 111 (1992).
Properties: mp 117-118°.
Melting point: mp 117-118°
Derivative Type: Hydrochloride
CAS Registry Number: 102676-31-3
Manufacturers' Codes: CGS-16949A
Trademarks: Afema (Novartis)
Molecular Formula: C14H13N3.HCl
Molecular Weight: 259.73
Percent Composition: C 64.74%, H 5.43%, N 16.18%, Cl 13.65%
Properties: Crystals from 2-propanol, mp 231-233°. Sol in water.
Melting point: mp 231-233°
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic (Hormonal); Aromatase Inhibitors; Aromatase Inhibitors.