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.
To a suspension of NaH (60%, 473 mg, 1 1.8 mmol) in DMF (5 mL) was added 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; 1.3 g, 5.91 mmol) at 0 C. The mixture was stirred for 5 min at 0 C and heated at 70 C for 30 min under nitrogen. The mixture was cooled to room temperature, a solution of 4-bromo-l-bromomethyl-2-fluoro-benzene (1.74 g, 6.5 mmol) in DMF (3 mL) was added and the mixture was stirred for 1.5 h at room temperature. Cold water (5 mL) was added. The mixture was extracted with EtOAc and the organic extract was dried (Na2S04), and evaporated. The residue was purified by chromatography (silica gel, 20% EtOAc/hexane) to give 2-(4-bromo-2-fluoro-benzyl)-6-tert-butyl-8-fluoro-2H-phthalazin-l-one (1.0 g, 41%) as a yellow solid. MS calcd. for Ci9Hi8BrF2N20 [(M+H)+] 407, obsd. 407.2., 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.
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;,
Phthalazine – Wikipedia
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