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A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines and Pharmaceuticals.

07:00 EST 29th January 2018 | BioPortfolio

Summary of "A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines and Pharmaceuticals."

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.

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This article was published in the following journal.

Name: Journal of the American Chemical Society
ISSN: 1520-5126
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Medical and Biotech [MESH] Definitions

Deuterium. The stable isotope of hydrogen. It has one neutron and one proton in the nucleus.

Hydrogen. The first chemical element in the periodic table. It has the atomic symbol H, atomic number 1, and atomic weight 1. It exists, under normal conditions, as a colorless, odorless, tasteless, diatomic gas. Hydrogen ions are PROTONS. Besides the common H1 isotope, hydrogen exists as the stable isotope DEUTERIUM and the unstable, radioactive isotope TRITIUM.

The isotopic compound of hydrogen of mass 2 (deuterium) with oxygen. (From Grant & Hackh's Chemical Dictionary, 5th ed) It is used to study mechanisms and rates of chemical or nuclear reactions, as well as biological processes.

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