MK 3814 is a potent and selective antagonist of the A(2a) receptor. A(2a) receptor antagonists have the potential for the treatment of Parkinson disease. Three distinct isotopically labelled forms of MK 3814 were synthesized. [H-3]MK 3814 was prepared for a preliminary absorption, distribution, metabolism, and excretion data (ADME) evaluation of the compound and [C-14]MK 3814 for more definitive ADME work, including an absorption, metabolism, and excretion study in man. In addition, [H-2(4)]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 H-3, H-2(4), and C-14-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 H-3, H-2(4), and C-14-MK 3814 (preladenant). Journal of Labelled Compounds and Radiopharmaceuticals, 60(4), 194-199. https://doi.org/10.1002/jlcr.3490