- Copper-catalyzed oxidative three-component synthesis of N, N′, N′-trisubstituted guanidines
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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
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- Addition of E-H (E = N, P, C, O, S) Bonds to Heterocumulenes Catalyzed by Benzimidazolin-2-iminato Actinide Complexes
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The synthesis and characterization of benzimidazolin-2-iminato actinide(IV) complexes [(BimR1/R2N)An(N{SiMe3}2)3] (An = U, Th) (1-6) is reported. All complexes were obtained in high yields, and their solid state structures were established through single-crystal X-ray diffraction analysis. Using 1-6 as precatalysts, the addition of mono- and bifunctional E-H (E = N, P, C, O, S) substrates to various heterocumulenes, including carbodiimides, isocyanates, and isothiocyanates, was investigated, affording the respective addition products in high yields under very mild reaction conditions. Various amines were applicable to this reaction, indicating a large scope capability of amine nucleophiles for the insertion process.
- Liu, Heng,Fridman, Natalia,Tamm, Matthias,Eisen, Moris S.
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supporting information
p. 3896 - 3903
(2017/10/30)
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- Synthesis of acylguanidine analogues: inhibitors of ADP-induced platelet aggregation
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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
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p. 228 - 236
(2007/10/02)
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