Triethylamine → HCID 52918885, compound

Participants

Reaction Steps

Thionyl chloride (0.23 mL) and dimethylformamide (0.01 mL) were added dropwise to a solution of Compound 2a (217 mg) obtained in Reference Example 1 and toluene (4 mL), and the mixture was stirred at 80° C. for 4.5 hours. After the resulting mixture was cooled, the solvents were evaporated. Without purification, the residual acid chloride was dissolved in dioxane (2 mL) to obtain a dioxane solution of acid chloride to be used in the following reaction. The dioxane solution of acid chloride was added dropwise under ice cooling to a solution of Compound 8a (100 mg) obtained in Reference Example 7 or Reference Example 8, triethylamine (0.01 mL) and dioxane (10 mL). The resulting mixture was stirred at room temperature for 8 hours, and the solvents were then evaporated. The resulting residue was purified by silica gel column chromatography (eluted with ethyl acetate/n-hexane (1:1)) to obtain Compound I-1 (119 mg).

Provenance & Evidence