反应详情

200 mg of water-moist Raney nickel and 0.2 ml of acetic acid are added to a solution of 122 mg (0.253 mmol) of 2-[3-(5-methyl-1,2,4-oxadiazol-3-yl)phenoxy]-N-[4-(2-oxopiperidin-1-yl)phenyl]-2-phenylacetamide in 5 ml of methanol, and the mixture is hydrogenated at room temperature and atmospheric pressure for 18 hours. The reaction mixture is filtered, and the residue is evaporated, giving 2-(3-amidinophenoxy)-N-[4-(2-oxopiperidin-1-yl)phenyl]-2-phenylacetamide, acetate (EMD 388547), ESI 443; IC50(Xa)=3.2×10−8 M; IC50(VIIa)=1.4×10−8 M.

1. customis hydrogenated at room temperature
2. filtrationThe reaction mixture is filtered
3. customthe residue is evaporated