With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1120-95-2,3-Chloropyridazine,as a common compound, the synthetic route is as follows.
(i?)-2-Methyl-l-{3-[4-(4,4,5,5-tetramethyl-[l,3,2]dioxaborolan-2-yl)- phenoxy]propyl} -pyrrolidine (1.1 g, 3.2 mmol), 3-chloropyridazine (0.485 g, 4.24 mmol) and tetrakis(triphenylphosphine)palladium(0) (0.258 g, 0.223 mmol), K2CO3 (1.19 g, 8.6 mmol) in 1,2-dimethoxyethane (25 mL) and water (11.5 mL) were combined and degassed with argon. The reaction was heated at 85 0C for 15 h, cooled to rt, filtered through celite, taken up in CH2Cl2 (30 mL) and washed with water and saturated NaHCO3 solution. The CH2Cl2 layer was dried (Na2SO4) and evaporated. The product was purified by ISCO chromatography on silica gel, eluting with 5-15% MeOH/ DCM / 0.5% NH4OH. The HCl salt was prepared MeOH – ether-HCl to give a white solid, m.p. 198-201 0C; LCMS m/z = 298 (M + 1).
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Reference£º
Patent; CEPHALON, INC.; WO2009/97306; (2009); A1;,
Pyridazine – Wikipedia
Pyridazine | C4H4N2 – PubChem