Selective N-monomethylation of primary anilines with the controllable installation of N-CH2D, N-CHD2, and N-CD3 units

Selective N-monomethylation of primary anilines with the controllable installation of N-CH2D, N-CHD2, and N-CD3 units

The selective N-monomethylation of primary anilines was realized by the use of the Me3N-BH3/N,N-dimethylformamide (DMF) system as the methyl source. This method also allows for the controllable introduction of N-CH2D, N-CHD2, and N-CD3 units with high levels of deuterium incorporation using Me3N-BH3...

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Veröffentlicht in:Organic & biomolecular chemistry 2020-07, Vol.18 (26), p.4922-4926
Hauptverfasser: Meng, Jing, Hui-Min, Xia, Ai-Qing, Xu, Yi-Feng, Wang, Wang, Zhijuan, Feng-Lian, Zhang
Format: Artikel
Sprache:eng
Schlagworte:
Aniline
CD3 antigen
Deuterium
Dimethylformamide
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Zusammenfassung:The selective N-monomethylation of primary anilines was realized by the use of the Me3N-BH3/N,N-dimethylformamide (DMF) system as the methyl source. This method also allows for the controllable introduction of N-CH2D, N-CHD2, and N-CD3 units with high levels of deuterium incorporation using Me3N-BH3/d7-DMF, Me3N-BD3/DMF and Me3N-BD3/d7-DMF systems, respectively.
ISSN:1477-0520
1477-0539
DOI:10.1039/d0ob01054e