triethylamine; benzylamine in chloroform T=55°C; 4 h; Reagent/catalystSolvent;

3-(3,5-bis-trifluoromethyl-phenylamino)-4-{[(S)-(6-methoxy-quinolin-4-yl)-((R)-5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methyl]-amino}-cyclobut-3-ene-1,2-dione in tert-butyl methyl ether T=45°C; Michael condensation; 8 h; optical yield given as percent eeenantioselective reaction;

3-(3,5-bis-trifluoromethyl-phenylamino)-4-{[(S)-(6-methoxy-quinolin-4-yl)-((R)-5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methyl]-amino}-cyclobut-3-ene-1,2-dione in tert-butyl methyl ether T=45°C; Michael condensation; 8 h; optical yield given as percent eeenantioselective reaction;

1H-imidazole; Magnesium acetate in tetrahydrofuran T=20°C; Claisen condensation; 17 h;

3-(3,5-bis-trifluoromethyl-phenylamino)-4-{[(S)-(6-methoxy-quinolin-4-yl)-((R)-5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methyl]-amino}-cyclobut-3-ene-1,2-dione in tert-butyl methyl ether T=45°C; Michael condensation; 60 h; optical yield given as percent eeenantioselective reaction;

3-(3,5-bis-trifluoromethyl-phenylamino)-4-{[(S)-(6-methoxy-quinolin-4-yl)-((R)-5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methyl]-amino}-cyclobut-3-ene-1,2-dione in tert-butyl methyl ether T=45°C; Michael condensation; 60 h; optical yield given as percent eeenantioselective reaction;