A common heterocyclic compound, the phthalazine compound, name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one,cas is 763111-47-3, mainly used in chemical industry, its synthesis route is as follows.,763111-47-3
4,4′-(((4,4′-(4,4′-(1,1,3,3-tetramethyldisiloxane-1,3-diyl)bis(butanoyl))bis(piperazine-4,1- diyl-1-carbonyl))bis(4-fluoro-3,1-phenylene))bis(methylene))bis(phthalazin-1(2H)-one): (0224) [3]: (0225) [00132] A solution of 4,4′-(1,1,3,3-tetramethyldisiloxane-1,3-diyl)dibutyric acid (250 mg, 0.816 mmol) in dichlromethane(5 mL) was charged EDCI-HCl (396 mg, 2.042 mmol) and 4-(4-fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one (598 mg, 1.633 mmol) at room temperature and stirred for 1hh. After completion of the reaction (monitored by TLC), water (5 mL) was added in the reaction mixture and organic layer was separated to obtain crude compound. The crude compound was purified by CombiFlash chromatography using 1-10% MeOH in DCM to obtain 286mg, 38% yield of the title compound as an off white solid.1H NMR (400 MHz, DMSO-d6): delta 12.57 (s, 2H), 8.55 (d, J = 10.27 Hz, 2H), 8.23 (d, J = 7.83 Hz, 1H), 7.92-7.96 (m, 1H), 7.84-7.89 (m, 2H), 7.78-7.83 (m, 2H), 7.38-7.44 (m, 2H), 7.33 (br. s, 2H), 7.21 (t, J = 8.80 Hz, 2H), 4.44 (s, 2H), 4.30 (s, 2H), 3.49-3.62 (m, 14H), 3.33-3.38 (m, 4H), 3.08-3.18 (m, 2H), 2.25-2.38 (m, 4H), 1.44-1.55 (m, 2H), 0.46-0.54 (m, 2H), 0.14 (br. s, 3H), 0.13 (br. s, 3H), 0.04 (br. s, 3H), 0.03 (br. s, 3H); MS (ES+): m/z = 493.20 [Monomer M – 18]+; LCMS: tR = 0.792 min.
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Reference£º
Patent; BLINKBIO, INC.; WANNER, Jutta; NGUYEN, Hanh, Nho; WERNER, Douglas, S.; OFORI, Leslie, Odame; (167 pag.)WO2017/214491; (2017); A1;,
Phthalazine – Wikipedia
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