Ethyl propiolate → HCID 68877294, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of the product from Step 5 (61 mg, 0.156 mmol) in DMF (2 mL) were added CuI (6 mg, 0.032 mmol) and TEA (45 μL, 0.323 mmol). The mixture was degassed with argon under sonication for 2-3 minutes and Pd(PPh3)4 (18 mg, 0.016 mmol) was added and the resulting mixture was heated at 55° C. for 15 min. Ethyl propiolate (4×5 μL, 0.197 mmol) was added to the reaction mixture at 55° C. in 30 minutes intervals. The crude mixture was concentrated and purified on silica gel with CH2Cl2/MeOH (100/1, 50/1, 25/1) as the eluents to afford 36 mg (64%) of the target compound.

Provenance & Evidence