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.
NaH (60%, 80 mg, 2 mmol) was added to a solution of 6-tert-butyl-8-fluoro-2H-phthalazin-l- one (which may be prepared as described in Berthel, S. et al. US 20100222325 Column 139; 220 mg, 1 mmol) in DMF (2 mL) at 0 C. The mixture was stirred for 5 min at 0 C and then heated at 70 C for 30 min. The mixture was cooled to room temperature, a solution of (5-bromo-2- bromomethyl-phenyl)-methanol (140 mg, 0.5 mmol) was added and the mixture was stirred for 1 h at room temperature. Ice-water (2 mL) was added. The mixture was extracted with EtOAc (3 x 25 mL). The EtOAc extract was washed with water (3 x 5 mL) and brine (5 mL), dried (Na2S04), filtered, and evaporated. The residue was purified by preparative HPLC to give 2-(4-bromo-2- hydroxymethyl-benzyl)-6-tert-butyl-8-fluoro-2H-phthalazin-l-one (62 mg, 15%) as a yellow gum. MS calcd. for C2oH2iBrFN202 [(M+H)+] 419, obsd. 418.8.
As the paragraph descriping shows that 1242156-59-7 is playing an increasingly important role.
Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; DOMINIQUE, Romyr; LOPEZ-TAPIA, Francisco Javier; MERTZ, Eric; SO, Sung-Sau; WO2014/76104; (2014); A1;,
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