A reliable one-pot synthesis of aryl azides from aryl amines using organotin azides as effective and recoverable reagents
A mild and mass-efficient procedure based on the one-pot diazotization-azidodediazoniation of aromatic amines is described. A wide range of aryl azides are obtained in moderate to high yields by using tributyltin azide as an effective and reusable azide source in the presence of p-toluenesulfonic acid at room temperature. The method was also successfully applied employing an insoluble polymer-supported organotin azide.
Godoy Prieto, Leonela,Lo Fiego, Marcos J.,Chopa, Alicia B.,Lockhart, María T.
Telescoped synthesis of C3-functionalized (E)-arylamidines using Ugi-Mumm and regiospecific quinazolinone rearrangements
An efficient four-step, six-transformation protocol was developed to afford bioactive N-alkyl- or N-arylamide (E)-arylamidines featuring strategic amidine C3 modifications which were inaccessible or low yielding by previous methods. This synthetic approac
Jaffett, Victor A.,Nerurkar, Alok,Cao, Xufeng,Guzei, Ilia A.,Golden, Jennifer E.
supporting information
p. 3118 - 3128
(2019/03/26)
Synthesis of Diverse Nitrogen Heterocycles via Palladium-Catalyzed Tandem Azide–Isocyanide Cross-Coupling/Cyclization: Mechanistic Insight using Experimental and Theoretical Studies
A rapid and elegant tandem azide–isocyanide cross-coupling/cyclization protocol has been developed based on a nitrene transfer reaction. The palladium-catalyzed ligand-free methodology led to the synthesis of three different heterocyclic scaffolds with excellent atom/step/redox economy. Studies based on first-principles-based quantum calculations and control experiments unraveled a concerted process of nitrene transfer reaction on isocyanides, ruling out the metallaaziridine intermediate reported earlier. This finding could pave the way for novel applications of nitrene transfer reactions to generate bioactive heterocycles. (Figure presented.).
USE OF CANNABINOID MODULATING COMPOUNDS IN COMBINATION WITH OTHER THERAPEUTIC COMPOUNDS FOR ADJUNCTIVE THERAPY
The present invention relates to pharmaceutical compositions that contain a compound that modulate the activity of a cannabinoid receptor in conjunction with another therapeutic compound and uses of compounds that modulate the activity of a cannabinoid re
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Page/Page column 299-300
(2008/12/04)
Efficient conversion of aromatic amines into azides: A one-pot synthesis of triazole linkages
An efficient and improved procedure for the preparation of aromatic azides and their application in the Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition ("click reaction") is described. The synthesis of aromatic azides from the corresponding amies i
Barral, Karine,Moorhouse, Adam D.,Moses, John E.
p. 1809 - 1811
(2008/02/02)
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