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A general strategy for site-selective incorporation of deuterium and tritium into pyridines, diazines, and pharmaceuticals
Koniarczyk, J. L., Hesk, D., Overgard, A., Davies, I. W., & McNally, A. (2018). A general strategy for site-selective incorporation of deuterium and tritium into pyridines, diazines, and pharmaceuticals. Journal of the American Chemical Society, 140(6), 1990-1993. https://doi.org/10.1021/jacs.7b11710
Methods to incorporate deuterium and tritium atoms into organic molecules are valuable for medicinal chemistry. The prevalence of pyridines and diazines in pharmaceuticals means that new Ways to label these heterocycles will present opportunities in drug design and facilitate absorption, distribution; metabolism, and excretion (ADME) studies. A broadly applicable protocol is presented wherein pyridines, diazines, and pharmaceuticals are converted into heterocyclic phosphonium salts and then isotopically labeled. The: isotopes are incorporated in high yields and, in general, with exclusive regioselectivity.
