15560-73-3Relevant academic research and scientific papers
Novel optimised quinuclidine squalene synthase inhibitors
Brown, George R.,Foubister, Alan J.,Freeman, Susan,McTaggart, Fergus,Mirrlees, Donald J.,Reid, Alan C.,Smith, Graham J.,Taylor, Melvyn J.,Thomason, Douglas A.,Whittamore, Paul R. O.
, p. 597 - 600 (1997)
Optimised quinuclidine squalene synthase (SQS) inhibitors are reported; 3-[2-(2-allyl-4-(2-ethoxy carbonylethyl)phenyl)ethynyl]quinuclidin-3-ol 1c, is a potent inhibitor of rat (KI = 6 nM) and human (KI = 43 nM) microsomal SQS; the oral ED50 of 1c, for the inhibition of rat cholesterol biosynthesis was 1.3 ± 0.45 mg/kg and for the R-enantiomer 1m, 0.8 ± 0.2 mg/kg, with the corresponding R-carboxylic acid 6a, being 0.9 ± 0.25 mg/kg.
MONO ET DIFLUORATION ELECTROCHIMIQUES DE GROUPES BENZYLIQUES
Laurent, Eliane,Marquet, Bernard,Tardivel, Robert
, p. 4431 - 4444 (2007/10/02)
Anodic oxidation of benzylic compounds 1 using CH3CN as a solvent and Et3N,3HF as a fluorinating reagent allowed to introduce a fluorine atom in α position of electron withdrawing group via carbocation 1+ (ECBECN mechanism).Whatever the E group, monofluorides 2 are obtained in good yields from paramethoxy derivatives 1 (R=p-OCH3).In this case, by raising the potential of working electrode after the monofluorination step, gem difluorides 3 can be directly prepared from 1.When the substituent of the phenyl ring is different of a methoxy group, a mixture of fluoride 2 and acetamide 4 is generally obtained and the ratio of these two compounds is related to cation stability.
