Synthesis of 3 H 3 3 H , 2 H 4 , 2 2 H 4 4 , and 14 C‐MK 14 14 C‐MK 3814 (preladenant)

摘要

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. [ 3 H]MK 3814 was prepared for a preliminary absorption, distribution, metabolism, and excretion data (ADME) evaluation of the compound and [ 14 C]MK 3814 for more definitive ADME work, including an absorption, metabolism, and excretion study in man. In addition, [ 2 H 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.