158641-45-3Relevant articles and documents
Synthesis of stable isotope labeled anacetrapib, its major metabolites and [14C]anacetrapib
Kuethe, Jeffrey T.,Soli, Eric D.,Royster, Pernilla,Quinn, Catherine A.
, p. 600 - 608 (2013)
Cholesteryl ester transfer protein inhibitors are an important class of compounds designed to treat hypocholesterolemia and prevent cardiovascular disease. Anacetrapib (MK-0859) is currently in phase III trials for the treatment of elevated cholesterol levels and prevention of cardiovascular disease. In order to further support the development of anacetrapib, we prepared [M + 6]MK-0859, which was required in support of an absolute bioavailability study of the active pharmaceutical ingredient (API). Additional support included the synthesis of an internal standard [M + 13] and three stable isotope labeled metabolites, which were used to analyze clinical samples, and [ 14C]MK-0859 to support drug metabolism studies. A labeling strategy for the preparation of [M + 6], [M + 13], and [14C]anacetrapib is described. The preparation of stable isotope labelled metabolites of anacetrapib is also described.
Synthesis and EPR Investigations of Fluorocatecholamines
Stegmann, Hartmut B.,Deuschle, Gabriele,Schuler, Paul
, p. 547 - 556 (2007/10/02)
The synthesis of 3-fluoro and 5-fluoronoradrenaline (3- and 5-fluoronorepinephrine) starting from 4-fluorophenol or 3-fluoroanisole is described.In the first step the second OH group is introduced followed by O-methylation and subsequent introduction of a
