A gold catalyzed enantioselective [3+2] dipolar cycloaddition of N-allenyl amides with nitrones was developed to give chiral 4-alkylidenyl isoxazolidine derivatives in high yields and excellent enantioselectivities by using BINOL derived chiral phosphoramidate Au(I) catalysts.
Gold(I) catalyzed [3+2] cycloaddition of azomethine imines with N-allenyl amides was developed to provide two types of pyrazolyl based bicyclic heterocycles. Both pyrazolidin-3-one derived and dihydroisoquinoline derived azomethine imines reacted smoothly with N-allenyl amides to give 6-methylene bipyrazolidin-1-ones and 1-methylene hexahydropyrazolo[5,1-a] isoquinolines in moderate to good yields.
1 May 2016 in International Journal of Pharmaceutics