反应详情

100 mg (0.52 mmol) of (S)-α-amino- N-[(1S,2S,4S)-1-(cyclohexylmethyl)-2-hydroxy-4-isopropyl-5-hexenyl]imidazole-4-propionamide and 0.052 ml of Hunig base in 2 ml of acetonitrile were treated at room temperature with 99 mg of N-(morpholinocarbamoyl)-3-phenyl-L-alanine and 113 mg of BOP in 2 ml of acetonitrile and stirred at room temperature for 12 hours. Thereafter, the reaction solution was poured onto 1N hydrochloric acid/ice, extracted with ethyl acetate, the organic extracts were dried over sodium sulfate and the solvent was removed under reduced pressure. The residue was chromatoqraphed on silica gel with a 10:1 mixture of methylene chloride and methanol, to obtain 130 mg (67%) of (S)-N-[(1S,2S,4S)-1-(cyclohexyl-methyl)-2-hydroxy-4-isopropyl-5 hexenyl]-α-2-[N-(morpholinocarbamoyl)-3-phenyl-L-alanyl]amino]imidazole-4-propionamide as an amorphous solid. MS: 651 (M+H)+.

1. extractionextracted with ethyl acetate
2. dry with materialthe organic extracts were dried over sodium sulfate
3. customthe solvent was removed under reduced pressure
4. additionThe residue was chromatoqraphed on silica gel with a 10:1 mixture of methylene chloride and methanol