反应详情

To a mixture of 2-amino-1,2,3,4-tetrahydro-naphthalene-2-carboxylic acid (4-diethylamino-phenyl)-amide (100 mg, 0.3 mmol) from Example 8 and N-Boc-glycine (52 mg, 0.3 mmol) in DMF (1.0 mL) was added Et3N (61 mg, 0.6 mmol) and TBTU (96 mg, 0.3 mmol). The mixture was stirred overnight and the precipitates were collected by filtration(130 mg) and dissolved in dichloromethane (10 mL) and TFA (5.0 mL). The mixture was concentrated under reduced pressure and ethyl acetate (20 mL) were added and the resulting solution was washed with 1N NaOH. The organic phase was dried over MgSO4 and then concentrated under reduced pressure to give 2-(2-amino-acetylamino)-1,2,3,4-tetrahydro-naphthalene-2-carboxylic acid (4-diethylamino-phenyl)-amide (70 mg).

1. filtrationthe precipitates were collected by filtration(130 mg)
2. dissolutiondissolved in dichloromethane (10 mL)
3. concentrationThe mixture was concentrated under reduced pressure and ethyl acetate (20 mL)
4. additionwere added
5. washthe resulting solution was washed with 1N NaOH
6. dry with materialThe organic phase was dried over MgSO4
7. concentrationconcentrated under reduced pressure