- A General and Mild Copper(I)-Catalyzed Three-Component Reaction of Cyanamides, Amines, and Diaryliodonium Triflates
-
A highly efficient copper-catalyzed three-component reaction of cyanamides, amines, and diaryliodonium triflates was developed for the synthesis of guanidines. The mild reaction accommodates both aromatic and aliphatic amines and provides the products in good yields with good functional group tolerance. Moreover, it was demonstrated that C-H activation of the arenes could be realized for the direct preparation of guanidines.
- Li, Jihui,Wang, Hongxing,Hou, Yifeng,Yu, Weiguang,Xu, Shuying,Zhang, Yucang
-
supporting information
p. 2388 - 2392
(2016/06/01)
-
- Copper-catalyzed oxidative three-component synthesis of N, N′, N′-trisubstituted guanidines
-
A copper-catalyzed three-component synthesis of trisubstituted N-aryl guanidines involving cyanamides, arylboronic acids, and amines has been developed. This operationally simple oxidative process, which is performed in the presence of K2CO3, a catalytic amount of CuCl 2·2H2O, bipyridine, and oxygen (1 atm), allows the rapid assembly of N,N′,N″-trisubstituted aryl guanidines.
- Li, Jihui,Neuville, Luc
-
supporting information
p. 6124 - 6127
(2014/01/17)
-
- Synthesis of acylguanidine analogues: inhibitors of ADP-induced platelet aggregation
-
Routine screening of compounds for inhibition of ADP-induced platelet aggregation in vitro revealed that 1'-hexamethylenebis[3-cyclohexyl-3-[(cyclohexylimino)(4-morpholinyl)methyl] urea] was active and represented the first example of a bis(acylguanidine) with possible antithrombotic activity. In order to develop a structure-activity relationship for this class of compounds, we synthesized a number of new bis(acylguanidines). These were tested in vitro, and several analogues were also active. Ex vivo testing revealed that compounds 22, 41, 58, and 70-73 were orally active in rats or guinea pigs.
- Thomas,Nishizawa,Zimmermann,Williams
-
p. 228 - 236
(2007/10/02)
-