MK 3814 is a potent and selective antagonist of the A2a receptor. A2a receptor 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.
Synthesis of 3H, 2H4, and 14C‐MK 3814 (preladenant)
Hesk, D., Borges, S., Dumpit, R., Hendershot, S., Koharski, D., Mcnamara, P., Ren, S., Saluja, S., Truong, V., & Voronin, K. (2017). Synthesis of 3H, 2H4, and 14C‐MK 3814 (preladenant). Journal of Labelled Compounds and Radiopharmaceuticals, 60(4), 194-199. https://doi.org/10.1002/jlcr.v60.4