Synthesis of 3 H, 13 C 2 , 2 H 4 14 C-SCH 430765 and 35 S-SCH 500946, potent and selective inhibitors of the NPY 5 receptor

• Published in: Journal of labelled compounds & radiopharmaceuticals Vol. 61; no. 7; pp. 533 - 539
• Main Authors: Hesk, D, Koharski, D, McNamara, P, Royster, P, Saluja, S, Truong, V, Voronin, K
• Format: Journal Article
• Language: English
• Published: England 15-06-2018
• Subjects: Carbon Isotopes; Carbon Radioisotopes; Chemistry Techniques, Synthetic; Isotope Labeling; Piperidines - chemical synthesis; Piperidines - chemistry; Piperidines - pharmacology; Radiochemistry; Receptors, Neuropeptide Y - antagonists & inhibitors; Sulfur Radioisotopes; Tritium; tritium exchange; carbon-14; sulphur-35; carbon-13; deuterium; iridium catalyst
• ISSN: 0362-4803; 1099-1344
• DOI: 10.1002/jlcr.3617

SCH 430765 and SCH 500496 are potent and selective antagonists of the NPY
receptor. NPY
receptor antagonists have the potential for the treatment of obesity. [
S]SCH 500946 was prepared for a competition binding assay which led to the identification of SCH 430765. Three distinct isotopically labelled forms of SCH 430765 were synthesized. [
H]SCH 430765 was prepared for a preliminary absorption, distribution, metabolism and excretion data evaluation of the compound and [
C]SCH 430765 for more definitive absorption, distribution, metabolism and excretion data work. In addition, [
C
,
H
]SCH 430765 was prepared as an internal standard for a LC-MS bioanalytical method. The paper discusses the synthesis of 3 isotopically labelled forms of SCH 430765 and [
S]SCH 500946.