title: Synthesis of3H,2H4, and14C-MK 3814 (preladenant).
abstract: MK 3814 is a potent and selective antagonist of the A2areceptor. A2areceptor antagonists have the potential for the treatment of Parkinson disease. Three distinct isotopically labelled forms of MK 3814 were synthesized. [3H]MK 3814 was prepared for a preliminary absorption, distribution, metabolism, and excretion data (ADME) evaluation of the compound and [14C]MK 3814 for more definitive ADME work, including an absorption, metabolism, and excretion study in man. In addition, [2H4]MK 3814 was prepared as an internal standard for a liquid chromatography mass spectrometry bioanalytical method. This paper discusses the synthesis of 3 isotopically labelled forms of MK 3814.
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: D
authors.identifier: 0000-0003-4059-4168
authors.initials: D
authors.lastname: Hesk
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: S
authors.initials: S
authors.lastname: Borges
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: R
authors.initials: R
authors.lastname: Dumpit
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: S
authors.initials: S
authors.lastname: Hendershot
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: D
authors.initials: D
authors.lastname: Koharski
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: P
authors.initials: P
authors.lastname: McNamara
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: S
authors.initials: S
authors.lastname: Ren
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: S
authors.initials: S
authors.lastname: Saluja
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: V
authors.initials: V
authors.lastname: Truong
authors.affiliation: Labeled Compound Synthesis, Merck & Co., Inc., Rahway, NJ, USA.
authors.forename: K
authors.initials: K
authors.lastname: Voronin
mesh_terms: D002250:Carbon Radioisotopes / Q000737:chemistry*; D060326:Chemistry Techniques, Synthetic; D003903:Deuterium / Q000737:chemistry*; D007553:Isotope Labeling; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry*; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry*; D014316:Tritium / Q000737:chemistry*
chemical_list: D002250:Carbon Radioisotopes; D011743:Pyrimidines; D014230:Triazoles; D014316:Tritium; C539997:2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7H-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine; D003903:Deuterium
keywords: carbon-14; deuterium; ruthenium catalyst; tritium exchange