volume 140 issue 6 pages 1990-1993

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

J Luke Koniarczyk 1
David Hesk 2
Alix Overgard 1
I.W Davies 2
2
 
Department of Process Research & Development, MRL, Merck Sharp & Dohme Corp., Rahway, New Jersey 07065, United States
Publication typeJournal Article
Publication date2018-02-05
scimago Q1
wos Q1
SJR5.554
CiteScore22.5
Impact factor15.6
ISSN00027863, 15205126
PubMed ID:  29377684
General Chemistry
Catalysis
Biochemistry
Colloid and Surface Chemistry
Abstract
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.
Found 
Found 

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GOST Copy
Koniarczyk J. L. et al. A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals // Journal of the American Chemical Society. 2018. Vol. 140. No. 6. pp. 1990-1993.
GOST all authors (up to 50) Copy
Koniarczyk J. L., Hesk D., Overgard A., Davies I., McNally A. A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals // Journal of the American Chemical Society. 2018. Vol. 140. No. 6. pp. 1990-1993.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1021/jacs.7b11710
UR - https://doi.org/10.1021/jacs.7b11710
TI - A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals
T2 - Journal of the American Chemical Society
AU - Koniarczyk, J Luke
AU - Hesk, David
AU - Overgard, Alix
AU - Davies, I.W
AU - McNally, Andrew
PY - 2018
DA - 2018/02/05
PB - American Chemical Society (ACS)
SP - 1990-1993
IS - 6
VL - 140
PMID - 29377684
SN - 0002-7863
SN - 1520-5126
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2018_Koniarczyk,
author = {J Luke Koniarczyk and David Hesk and Alix Overgard and I.W Davies and Andrew McNally},
title = {A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals},
journal = {Journal of the American Chemical Society},
year = {2018},
volume = {140},
publisher = {American Chemical Society (ACS)},
month = {feb},
url = {https://doi.org/10.1021/jacs.7b11710},
number = {6},
pages = {1990--1993},
doi = {10.1021/jacs.7b11710}
}
MLA
Cite this
MLA Copy
Koniarczyk, J. Luke, et al. “A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals.” Journal of the American Chemical Society, vol. 140, no. 6, Feb. 2018, pp. 1990-1993. https://doi.org/10.1021/jacs.7b11710.