title: Synthesis of stable isotope labeled anacetrapib, its major metabolites and [(14) C]anacetrapib.
abstract: 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 [(14) C]MK-0859 to support drug metabolism studies.
authors.affiliation: Department of Process Chemistry, Labeled Compound Synthesis Group, Merck & Co., Inc, Rahway, New Jersey, 07065, USA.
authors.forename: Jeffrey T
authors.initials: JT
authors.lastname: Kuethe
authors.forename: Eric D
authors.initials: ED
authors.lastname: Soli
authors.forename: Pernilla
authors.initials: P
authors.lastname: Royster
authors.forename: Catherine A
authors.initials: CA
authors.lastname: Quinn
mesh_terms: D000924:Anticholesteremic Agents / Q000138:chemical synthesis*; D002250:Carbon Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling; D023303:Oxazolidinones / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
chemical_list: D000924:Anticholesteremic Agents; D002250:Carbon Radioisotopes; D023303:Oxazolidinones; D019275:Radiopharmaceuticals; C530884:anacetrapib
keywords: CETP; MK-0859; anacetrapib; internal standard