反应详情

温度

100 °C

To a solution of [2-chloro-4-fluoro-phenyl]methyl isocyanide (0.068 g, 0.4 mmol) and succinic semialdehyde (15% in water, 0.26 ml, 0.4 mmol) in methanol (1.75 ml) was added cyclopropylamine (0.042 ml, 0.6 mmol). The mixture was heated to 100° C. for 30 minutes in a microwave reactor. The solvent was removed in vacuo and the residue was purified by mass-directed automated HPLC to give a colourless gum which was triturated with diethyl ether to give N-[(2-chloro-4-fluorophenyl)methyl]-1-cyclopropyl-5-oxoprolinamide as a pale cream solid (0.058 g). LC/MS [M+H]+=310, retention time=2.16 minutes.

1. customThe solvent was removed in vacuo
2. customthe residue was purified
3. customto give a colourless gum which
4. customwas triturated with diethyl ether