With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.75884-70-7,6-Bromophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.
6-Bromophthalazin-1(2H)-one (1.00 g, 4.44 mmol), cyclopropylboronic acid (0.57 g, 6.67 mmol), tricyclohexylphosphine (0.13 g, 0.44 mmol) and potassium phosphate (0.57 g, 6.67 mmol) were suspended in a mixed solution of toluene (20mL) and water (1mL). To this mixture, palladium(II) acetate (0.20 g, 0.89 mmol) was added under nitrogen atmosphere at ambient temperature and stirred at 100 C for 3 h. Cooled to ambient temperature, the reaction mixture was filtered and insoluble material was washed with water and ethyl acetate. The filtrate was extracted with ethyl acetate, washed with water and brine, dried over sodium sulfate, filtered and concentrated. The crude material was purified by chromatography on silica gel, eluted with hexane/ethyl acetate to afford 6-cyclopropylphthalazin-1(2H)-one (0.13 g). 1H NMR (400 MHz, DMSO-d6) delta 12.52 (s, 1H), 8.25 (s, 1H), 8.08 (d, J = 8.2 Hz, 1H), 7.60 (d, J = 1.7 Hz, 1H), 7.56 (dd, J = 8.3, 1.8 Hz, 1H), 2.18 – 2.00 (m, 1H), 1.14 – 1.08 (m, 2H), 0.89 – 0.83 (m, 2H) ; LCMS (m/z): 187.1 [M+H]+.
As the paragraph descriping shows that 75884-70-7 is playing an increasingly important role.
Reference£º
Patent; Carna Biosciences, Inc.; KAWAHATA, Wataru; ASAMI, Tokiko; SAWA, Masaaki; ASAMITSU, Yuko; IRIE, Takayuki; MIYAKE, Takahiro; KIYOI, Takao; EP2824099; (2015); A1;,
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