反应详情

To a solution of compound 1 (400 mg) in CH2Cl2 (10 mL) was added triphosgene (1.0 eq.) and triethylamine (2.5 eq.) at 0° C. The reaction mixture was stirred for 2 h. at r. t and morpholine (3.0 eq.) was added. The reaction was stirred until it appeared by TLC to be completed (˜4 h), and was washed with 1N HCl and sat NaHCO3 (3×10 mL). The solvents were removed by evaporation under reduced pressure to give product 16 (520 mg). The crude product appeared to be pure by TLC and NMR and used for the next step reaction without further purification.

1. stirringThe reaction was stirred until it
2. custom(˜4 h)
3. washwas washed with 1N HCl
4. customThe solvents were removed by evaporation under reduced pressure