Diisopropylethylamine → HCID 178495256, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of (2E)-3-(dimethylamino)-1-{4-[1-(2-methoxypropyl)-1H-1,2,4-triazol-5-yl]-9-oxa-3,6-diazatricyclo[8.4.0.02,6]tetradeca1(14),2,4,10,12-pentaen-12-yl}prop-2-en-1-one (105 mg, 0.250 mmol), tert-butyl 4-hydrazinylpiperidine-1-carboxylate (108 mg, 0.500 mmol), and DIPEA (60 mg, 0.50 mmol) in ethanol (10 mL) was stirred at 80° C. for 48 h under nitrogen atmosphere. After concentration, the residue was purified by reverse phase Combiflash eluting with a 0-40% gradient of CH3CN in 0.3% NH4HCO3 to give 1-tert-butyl-6-(5-{4-[1-(2-methoxypropyl)-1H-1,2,4-triazol-5-yl]-9-oxa-3,6-diazatricyclo[8.4.0.02,6]tetradeca1(14),2,4,10,12-pentaen-12-yl}-1H-pyrazol-1-yl)-1λ3,3-oxazocan-2-one (105 mg, 67% yield). LCMS (ESI) m/z: 422.1 [M+H+].

Provenance & Evidence