Synthetic Route of 94220-45-8 , The common heterocyclic compound, 94220-45-8, name is 5-Chloro-1H-pyrazolo[4,3-b]pyridine, molecular formula is C6H4ClN3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
To a solution of 5-chloro-1H-pyrazolo[4,3-b]pyridine (500 mg, 3.29 mmol) in 1,4-dioxane (20 mL) and water (5 mL) were added (2-fluorophenyl)boronic acid (500 mg, 3.57 mmol), potassium phosphate (1.4 g, 6.5 mmol) and (2′-aminobiphenyl-2-yl)(chloro)(dicyclohexyl(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphoranylidene)palladium (100 mg, 0.127 mmol). The reaction was degassed and backfilled with N2 and stirred at 90 C. for 15 hours. After this time it was cooled to r.t., filtered and concentrated to dryness. The residue was purified by silica gel chromatography using 0-100% ethyl acetate in hexanes to afford desired product as yellowish oil (620 mg, 98%). LC-MS calculated for C12H9FN3 (M+H)+: m/z=214.2; found 214.2.
The synthetic route of 94220-45-8 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Incyte Corporation; Liu, Kai; Pan, Jun; Sokolsky, Alexander; Vechorkin, Oleg; Ye, Hai Fen; Ye, Qinda; Yao, Wenqing; (75 pag.)US2018/72718; (2018); A1;,
Pyridine – Wikipedia,
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