volume 65 issue 4 pages 757-764

An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate

Rémy Morgentin 1
Frédéric Jung 1
Maryannick Lamorlette 1
Mickaël Maudet 1
Morgan Ménard 1
Patrick Plé 1
Georges Pasquet 1
F. Renaud 1
1
 
AstraZeneca, Centre de Recherches, Parc industriel Pompelle B.P. 1050, 51689 Reims cedex 2, France
Publication typeJournal Article
Publication date2009-01-01
scimago Q3
wos Q2
SJR0.426
CiteScore4.1
Impact factor2.2
ISSN00404020, 14645416
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
The synthesis of methyl 2-(5-hydroxy-3-methoxypyridin-2-yl)acetate and alkyl 2-(5-hydroxypyrimidin-2-yl)acetate is described. Methodology for an efficient access to 5-hydroxy-pyridin- and pyrimidin-2-yl acetate cores has been developed. Based on the difference in halogen reactivity, 5-bromo-2-chloropyridine and its pyrimidine analogue were functionalized judiciously by SNAr and palladium-catalyzed reactions. The outlined strategy provides a high-yielding route suitable for large-scale synthesis of these compounds as well as paves the way for a potential rapid access to other heterocyclic analogues.
Found 
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GOST Copy
Morgentin R. et al. An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate // Tetrahedron. 2009. Vol. 65. No. 4. pp. 757-764.
GOST all authors (up to 50) Copy
Morgentin R., Jung F., Lamorlette M., Maudet M., Ménard M., Plé P., Pasquet G., Renaud F. An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate // Tetrahedron. 2009. Vol. 65. No. 4. pp. 757-764.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.tet.2008.11.064
UR - https://doi.org/10.1016/j.tet.2008.11.064
TI - An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate
T2 - Tetrahedron
AU - Morgentin, Rémy
AU - Jung, Frédéric
AU - Lamorlette, Maryannick
AU - Maudet, Mickaël
AU - Ménard, Morgan
AU - Plé, Patrick
AU - Pasquet, Georges
AU - Renaud, F.
PY - 2009
DA - 2009/01/01
PB - Elsevier
SP - 757-764
IS - 4
VL - 65
SN - 0040-4020
SN - 1464-5416
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2009_Morgentin,
author = {Rémy Morgentin and Frédéric Jung and Maryannick Lamorlette and Mickaël Maudet and Morgan Ménard and Patrick Plé and Georges Pasquet and F. Renaud},
title = {An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate},
journal = {Tetrahedron},
year = {2009},
volume = {65},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/j.tet.2008.11.064},
number = {4},
pages = {757--764},
doi = {10.1016/j.tet.2008.11.064}
}
MLA
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MLA Copy
Morgentin, Rémy, et al. “An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate.” Tetrahedron, vol. 65, no. 4, Jan. 2009, pp. 757-764. https://doi.org/10.1016/j.tet.2008.11.064.