A chemoselective aniline-chloropyrimidine coupling in a competing electrophilic environment
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作者:
Choudhury, Anusuya
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LLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USALLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USA
Choudhury, Anusuya
[1
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Chen, Hongfeng
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LLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USALLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USA
Chen, Hongfeng
[1
]
Nilsen, Christopher N.
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LLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USALLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USA
Nilsen, Christopher N.
[1
]
Sorgi, Kirk L.
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LLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USALLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USA
Sorgi, Kirk L.
[1
]
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[1] LLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USA
A highly chemoselective substitution on 4-amino-6-chloropyrimidine ring system having a competing aldehyde functionality has been realized with anilines which produces 4, 6-diaminopyrimidine-5-carbaldehyde in high yield. The reaction may involve the intermediacy of imines. A variety of aromatic amines participate in this reaction successfully to generate diaminopyrimidine aldehydes in moderate to high yield. (C) 2007 Elsevier Ltd. All rights reserved.