Title: Avasimibe
CAS Registry Number: 166518-60-1
CAS Name: [[2,4,6-Tris(1-methylethyl)phenyl]acetyl]sulfamic acid 2,6-bis(1-methylethyl)phenyl ester
Additional Names: 2,6-diisopropylphenyl[(2,4,6-triisopropylphenyl)acetyl]sulfamate
Manufacturers' Codes: CI-1011; PD-148515
Molecular Formula: C29H43NO4S
Molecular Weight: 501.72
Percent Composition: C 69.42%, H 8.64%, N 2.79%, O 12.76%, S 6.39%
Literature References: Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor. Prepn: H. T. Lee et al., WO 9426702; eidem, US 5491172 (1994, 1996 both to Warner Lambert). Scale up synthesis: G. J. Dozeman et al, Org. Process Res. Dev. 1, 137 (1997). ACAT inhibition studies: H. T. Lee et al., J. Med. Chem. 39, 5031 (1996). HPLC/MS/MS determn in plasma: W. W. Bullen et al., J. Pharm. Biomed. Anal. 17, 1399 (1998). Clinical evaluation in hyperlipidemia: W. Insull Jr. et al., Atherosclerosis 157, 137 (2001). Toxicology: D. G. Robertson et al., Toxicol. Sci. 59, 324 (2001). Reviews of development and therapeutic potential: R. Jones, Curr. Opin. Cardiovasc. Pulmon. Renal Invest. Drugs 1, 263-269 (1999); idem, ibid. 2, 274-278 (2000).
Properties: White solid, mp 178-180° (Lee). Also reported as white powder, mp 169.5-170.4° (Dozeman).
Melting point: mp 178-180° (Lee); mp 169.5-170.4° (Dozeman)
Derivative Type: Sodium salt
CAS Registry Number: 166518-61-2
Properties: White solid, mp 250-252°.
Melting point: mp 250-252°
Therap-Cat: Antilipemic.
Keywords: Antilipemic. |