反应详情

To a premixed solution of trimethyl acetyl chloride (240 mg, 2.0 mmol) and triethylamine (0.35 ml, 2.5 mmol) was added 2-{3-[2-fluoro-5-(4-oxo-3,4-dihydro-phthalazin-1-ylmethyl)-phenyl]-urido}-propionic acid (45)(0.76 g, 2.0 mmol). The reaction was stirred at room temperature for 4 days at room temperature with slow progression to the desired product. The reaction mixture was then concentrated in vacuo and the crude material was submitted for preparative HPLC (40 mg isolated, 95% purity, RT (mins): 4.35)