Title: Torcetrapib
CAS Registry Number: 262352-17-0
CAS Name: (2R,4S)-4-[[[3,5-Bis(trifluoromethyl)phenyl]methyl](methoxycarbonyl)amino]-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-1(2H)-quinolinecarboxylic acid ethyl ester
Additional Names: (2R,4S)-4-[(3,5-bis-trifluoromethylbenzyl)methoxycarbonylamino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester
Manufacturers' Codes: CP-529414
Molecular Formula: C26H25F9N2O4
Molecular Weight: 600.47
Percent Composition: C 52.01%, H 4.20%, F 28.48%, N 4.67%, O 10.66%
Literature References: Cholesteryl ester transfer protein (CETP) inhibitor. Prepn: M. P. DeNinno et al., WO 0017164; eidem, US 6197786 (2000, 2001 both to Pfizer); of crystalline forms: D. J. M. Allen et al., WO 0140190 (2001 to Pfizer). Mechanism of action study: R. W. Clark et al., J. Lipid Res. 47, 537 (2006). Clinical evaluation of effects on HDL cholesterol levels: R. W. Clark et al., Arterioscler. Thromb. Vasc. Biol. 24, 490 (2004); M. E. Brousseau et al., N. Engl. J. Med. 350, 1505 (2004). Review of clinical development in combination with atorvastatin: J. R. Burnett, Curr. Opin. Invest. Drugs 6, 944-950 (2005).
Properties: Anhydrous, non-hygroscopic crystals, mp 89-90°. d 1.406.
Melting point: mp 89-90°
Density: d 1.406
Derivative Type: Ethanolate
CAS Registry Number: 343798-00-5
Molecular Formula: C26H25F9N2O4.C2H6O
Molecular Weight: 646.54
Percent Composition: C 52.02%, H 4.83%, F 26.45%, N 4.33%, O 12.37%
Properties: White crystalline powder, mp 54-58°. [a]D -93.3° (c = 1.08 in methanol). d 1.402. Non-hygroscopic. Higher aqueous soly than anhydrous form.
Melting point: mp 54-58°
Optical Rotation: [a]D -93.3° (c = 1.08 in methanol)
Density: d 1.402
Therap-Cat: Antilipemic; antiatherosclerotic.
Keywords: Antilipemic; CETP Inhibitor; Antiatherosclerotic. |