With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1242156-59-7,6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.
Under N2, acetic acid 2,6-dibromobenzyl ester (24.74 g, 80.3 mmol), 6-tert-butyl-8-fluoro-2H-phthazin-1-one (3.54 g, 16.1 mmol), Cs2CO3 (10.46 g, 32.1 mmol), CuI (4.61 g, 24.2 mmol) and N,N-dimethylethane-1,2-diamine (1.42 g, 16.1 mmol) were dissolved in DMF (70 mL). The reaction mixture was stirred at 150 C. for 4 h. The resulting mixture was cooled to room temperature and diluted with ethyl acetate (200 mL), and then 200 mL of water was added. The mixture was separated and the aqueous layer was extracted with ethyl acetate (200 mL¡Á2). The organic layers were combined and washed with water (200 mL) and brine (200 mL). The solution was dried over anhydrous sodium sulfate, filtered and concentrated. The resulting crude product was purified by silica gel chromatography (petroleum ether/ethyl acetate 4/1) to give 2-bromo-6-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-benzyl ester (3.21 g, 45%). 1H NMR (300 MHz, CDCl3): delta 8.17 (d, J=2.7 Hz, 1H), 7.71 (t, J=4.8 Hz, 1H), 7.50-7.45 (m, 2H), 7.36 (s, 1H), 7.34 (d, J=0.9 Hz, 1H), 5.17 (s, 2H), 1.94 (s, 3H), 1.42 (s, 9H). LC-MS calcd for C21H20BrFN2O3 (m/e) 446.06, obsd 447 and 449 [M+1]+., 1242156-59-7
1242156-59-7 6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one 59473765, aphthalazine compound, is more and more widely used in various fields.
Reference£º
Patent; Billedeau, Roland Joseph; Kondru, Rama K.; Lopez-Tapia, Francisco Javier; Lou, Yan; Owens, Timothy D.; Qian, Yimin; So, Sung-Sau; Thakkar, Kshitij C.; Wanner, Jutta; US2012/295885; (2012); A1;,
Phthalazine – Wikipedia
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