期刊
CHEMISTRY-AN ASIAN JOURNAL
卷 18, 期 1, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.202201006
关键词
Copper; Dialkylamination; chloroheteroarenes; SNAr amination; N; N-dimethylformamide (DMF)
In this study, a highly efficient room-temperature dimethylamination of chloroheteroarenes was achieved by in-situ generation of dimethylamine using N,N-dimethylformamide (DMF) as a precursor. The reaction exhibited a broad substrate scope, including various heteroarenes and commercially relevant drugs.
The dimethylamino functionality has significant importance in industrially relevant molecules and methodologies to install these efficiently are highly desirable. We report herein a highly efficient, room-temperature dimethylamination of chloroheteroarenes performed via the in-situ generation of dimethylamine using N,N-dimethylformamide (DMF) as precursor wiith a large substrate scope that includes various heteroarenes, purines as well as commercially relevant drugs such as altretamine, ampyzine and puromycin precursor.
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