反应详情

This compound was prepared according to a procedure similar to that described in Procedure H. In a solution of 9-Bromo-4,5-dihydro-6-oxa-1,3a-diaza-benzo[e]azulene-2-carboxylic acid amide (100 mg, 0.32 mmol) in N,N-Dimethyl-formamide (3 mL) were added 1,3-bis(diphenylphosphino)-propane (26 mg, 0.064 mmol), Pd(OAc)2 (7.2 mg, 0.032 mmol), K2CO3 (110 mg, 0.8 mmol), 3-Ethynyl-3-hydroxy-pyrrolidine-1-carboxylic acid tert-butyl ester (136 mg, 0.64 mmol) and CuI (12 mg, 0.064 mmol). Then the solution was bubbled N2 for 5 min and microwaved for 1 h at 120° C. under nitrogen. The reaction mixture was filtrated and the filtrate was purified by column to afford crude titled compound (40 mg, 28%). LCMS=383.0 [M-56]+.

1. customThis compound was prepared
2. customThen the solution was bubbled N2 for 5 min
3. custommicrowaved for 1 h at 120° C. under nitrogen
4. filtrationThe reaction mixture was filtrated
5. customthe filtrate was purified by column