Streamlining amine synthesis

• Published in: Science (American Association for the Advancement of Science) Vol. 348; no. 6237; pp. 863 - 864
• Main Author: Kuerti, Laszlo
• Format: Journal Article
• Language: English
• Published: Washington The American Association for the Advancement of Science 22-05-2015
• Subjects: Amines; Atoms & subatomic particles; Chemists; Derivatives; Nitrogen; Nitrogen atoms; Olefins; Organic compounds; Organisms; Synthesis
• ISSN: 0036-8075; 1095-9203
• DOI: 10.1126/science.aab2812

Bulky amine groups that help make many drugs more bioavailable can be added readily to organic compounds
[Also see Research Article by
Gui
et al.
]
Amines, a collective name for compounds that contain one or more nitrogen atoms, and their derivatives make up the overwhelming majority of drug molecules and agrochemicals, as well as many compounds that are produced by plants and living organisms (i.e., natural products) (
1
,
2
). Not surprisingly, organic chemists spend a considerable amount of time with the synthesis and late-stage functionalization of amines. On page 886 of this issue, Gui
et al.
(
3
) report a highly innovative iron-catalyzed cross-coupling of olefins with nitroarenes, both of which are readily available and inexpensive, to afford bulky secondary arylamines that are either very difficult to obtain or inaccessible with existing methods.