Organic Process Research and Development, volume 13, issue 3, pages 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.
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Publication type: Journal Article
Publication date: 2009-04-27
scimago Q1
SJR: 0.900
CiteScore: 6.9
Impact factor: 3.1
ISSN: 10836160, 1520586X
Organic Chemistry
Physical and Theoretical Chemistry
Abstract
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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