American Chemical Society (ACS)
Organic Process Research and Development
,  том 13 ,  издание 3 ,  страницы 652-655

An Efficient Synthetic Process for Scale-Up Production of 4,5-Diamino-2-(trifluoromethyl)benzonitrile and 5-Bromo-3-(trifluoromethyl)benzene-1,2-diamine

Xun Li 1
, 
Raymond A Ng 1
, 
Yongzheng Zhang 1
, 
Ronald K Russell 1
, 
Zhihua Sui 1
1
 
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., East Coast Research & Early Development, 1000 Route 202, Raritan, New Jersey 08869 U.S.A. | 
Тип публикации: Journal Article
Дата публикации: 2009-04-27
American Chemical Society (ACS)
scimago Q1
wos Q1
БС1
SJR: 0.865
CiteScore: 5.4
Impact factor: 3.5
ISSN: 10836160, 1520586X
Organic Chemistry
Physical and Theoretical Chemistry
Краткое описание
Starting from 4-amino-2-(trifluoromethyl)benzonitrile (6), an efficient and nonchromatographic process was developed for multihundred gram production of 4,5-diamino-2-(trifluoromethyl)benzonitrile (1) in 73% yield and 98 HPLC area% purity over four synthetic steps. The same synthetic strategy was applied to 4-bromo-2-(trifluoromethyl)aniline (7) that afforded 5-bromo-3-(trifluoromethyl)benzene-1,2-diamine (5) in 81% overall yield and 99% HPLC area% purity.
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Li X. et al. An Efficient Synthetic Process for Scale-Up Production of 4,5-Diamino-2-(trifluoromethyl)benzonitrile and 5-Bromo-3-(trifluoromethyl)benzene-1,2-diamine // Organic Process Research and Development. 2009. Vol. 13. No. 3. pp. 652-655.
ГОСТ со всеми авторами (до 50) Скопировать
Li X., Ng R. A., Zhang Y., Russell R. K., Sui Z. An Efficient Synthetic Process for Scale-Up Production of 4,5-Diamino-2-(trifluoromethyl)benzonitrile and 5-Bromo-3-(trifluoromethyl)benzene-1,2-diamine // Organic Process Research and Development. 2009. Vol. 13. No. 3. pp. 652-655.
RIS |
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TY - JOUR
DO - 10.1021/op9000498
UR - https://doi.org/10.1021/op9000498
TI - An Efficient Synthetic Process for Scale-Up Production of 4,5-Diamino-2-(trifluoromethyl)benzonitrile and 5-Bromo-3-(trifluoromethyl)benzene-1,2-diamine
T2 - Organic Process Research and Development
AU - Li, Xun
AU - Ng, Raymond A
AU - Zhang, Yongzheng
AU - Russell, Ronald K
AU - Sui, Zhihua
PY - 2009
DA - 2009/04/27
PB - American Chemical Society (ACS)
SP - 652-655
IS - 3
VL - 13
SN - 1083-6160
SN - 1520-586X
ER -
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@article{2009_Li,
author = {Xun Li and Raymond A Ng and Yongzheng Zhang and Ronald K Russell and Zhihua Sui},
title = {An Efficient Synthetic Process for Scale-Up Production of 4,5-Diamino-2-(trifluoromethyl)benzonitrile and 5-Bromo-3-(trifluoromethyl)benzene-1,2-diamine},
journal = {Organic Process Research and Development},
year = {2009},
volume = {13},
publisher = {American Chemical Society (ACS)},
month = {apr},
url = {https://doi.org/10.1021/op9000498},
number = {3},
pages = {652--655},
doi = {10.1021/op9000498}
}
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Li, Xun, et al. “An Efficient Synthetic Process for Scale-Up Production of 4,5-Diamino-2-(trifluoromethyl)benzonitrile and 5-Bromo-3-(trifluoromethyl)benzene-1,2-diamine.” Organic Process Research and Development, vol. 13, no. 3, Apr. 2009, pp. 652-655. https://doi.org/10.1021/op9000498.