Diisopropylethylamine → HCID 178453343, compound

Participants

Reaction Conditions

Reaction Steps

3-Aminopyrazole (92 mg, 1.08 mmol) and DIEA (110 μL, 1.08 mmol) were added to a solution of compound 57-b (0.31 mmol) in anh. DMF (3 mL). The solution was cooled to 0° C. and stirred for 2-3 minutes, then HATU (126 mg, 0.32 mmol) in anh. DMF (1 mL) was added. The reaction mixture was allowed to attain room temperature, stirred for 16 h and then diluted with DCM. The organic phase was extracted with NaHCO3 sat. aq. solution. The aqueous phase was extracted with ethyl acetate and the combined organics dried over anh. Na2SO4 and then concentrated. Purification by flash column chromatography (MeOH/DCM, 0:1-2:8) gave the title compound (91 mg g, 63%). MS m/z 468.3 (M+H)+.

Provenance & Evidence