反应详情

KY-767-batch-A To a solution of (E)-3-azido-2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl)hydrazono) propanoic acid (E)-KY-757, (100 mg) in CH3CN 1 ml, tert-butanol 0.4 ml was added diisopropylethylamine 96 ul followed by 2-ethynylpyridine (0.4 mmol, 41 ul), CuI (15 mg). The reaction stirred at rt for 3 h. LC-MS assay showed two isomers. The solvent was removed under pressure. The residue was purified on C18 reversed phase flash chromatography column employing a linear gradient of 0-30% A in B (flow rate 40 ml/min), were A is 10% NH4OH in CH3CN and B is water, yielding (14 mg, 18%) of pure (E)-KY-788. MS+(ESI) m/z 373.91, calcd mass 473.85.

1. customThe solvent was removed under pressure
2. customThe residue was purified on C18 reversed phase flash chromatography column
3. customyielding (14 mg, 18%) of pure (E)-KY-788