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One-Pot Synthesis of Ureas from Boc-Protected Amines

Constantinos Spyropoulos and Christoforos G. Kokotos*

*Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis 15771, Athens, Greece, Email:

C. Spyropoulos, C. G. Kokotos, J. Org. Chem., 2014, 79, 4477-4483.

DOI: 10.1021/jo500492x


In a practical one-pot synthesis of ureas, Boc-protected amines are transformed into nonsymmetrical and symmetrical disubstituted and trisubstituted ureas via in situ generation of isocyanates utilizing 2-chloropyridine and trifluoromethanesulfonyl anhydride. A variety of amines can be employed successfully, leading to high yields of isolated ureas.

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Key Words

Ureas, Boc-protected Amines

ID: J42-Y2014