Organic Process Research and Development, volume 22, issue 2, pages 166-172
Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones
1
Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States
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2
Wuxi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China
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Publication type: Journal Article
Publication date: 2018-01-11
Quartile SCImago
Q1
Quartile WOS
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Impact factor: 3.4
ISSN: 10836160, 1520586X
Organic Chemistry
Physical and Theoretical Chemistry
Abstract
The synthesis of a series of imidazo[5,1-f][1,2,4]triazin-4(3H)-ones was developed from starting imidazoles in three linear steps. The synthetic sequence began with an electrophilic amination and thus a rigorous campaign to identify safe reagent and reaction conditions was performed to ensure safety for preparation of these versatile intermediates on large scales. Functionalizations at the key positions on these substrates were exemplified to demonstrate ability to perform late-stage diversification for efficient SAR discovery.
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Tran T. P. et al. Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones // Organic Process Research and Development. 2018. Vol. 22. No. 2. pp. 166-172.
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Tran T. P., Fisher E. L., Wright A. S., Jiao Y. Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones // Organic Process Research and Development. 2018. Vol. 22. No. 2. pp. 166-172.
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TY - JOUR
DO - 10.1021/acs.oprd.7b00333
UR - https://doi.org/10.1021/acs.oprd.7b00333
TI - Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones
T2 - Organic Process Research and Development
AU - Wright, Ann S
AU - Jiao, Yang
AU - Tran, Tuan P
AU - Fisher, Ethan L
PY - 2018
DA - 2018/01/11
PB - American Chemical Society (ACS)
SP - 166-172
IS - 2
VL - 22
SN - 1083-6160
SN - 1520-586X
ER -
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@article{2018_Tran,
author = {Ann S Wright and Yang Jiao and Tuan P Tran and Ethan L Fisher},
title = {Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones},
journal = {Organic Process Research and Development},
year = {2018},
volume = {22},
publisher = {American Chemical Society (ACS)},
month = {jan},
url = {https://doi.org/10.1021/acs.oprd.7b00333},
number = {2},
pages = {166--172},
doi = {10.1021/acs.oprd.7b00333}
}
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MLA
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Tran, Tuan P., et al. “Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones.” Organic Process Research and Development, vol. 22, no. 2, Jan. 2018, pp. 166-172. https://doi.org/10.1021/acs.oprd.7b00333.