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HRID 79382作成日:2026年10月25日

Potassium Carbonate → N-(3-ethyl-1-((6-methylpyridin-2-yl)methyl)-1H-indazol-4-yl)-7-(5,6,7,8-tetrahydroimidazo[1,2-a]pyrazin-3-yl)imidazo[1,2-a]pyridine-3-carboxamide

https://huagongshe.com/reaction/79382

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物tert-Butyl 5,6-dihydroimidazo(1,2-a)pyrazine-7(8H)-carboxylateHCID 21955306—
反応物7-Bromo-N-(3-ethyl-1-((6-methylpyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamideHCID 67259557—
触媒palladium(II) acetateHCID 167845—
触媒HCID 178418397HCID 178418397—
溶媒DimethylformamideHCID 6228—
生成物N-(3-ethyl-1-((6-methylpyridin-2-yl)methyl)-1H-indazol-4-yl)-7-(5,6,7,8-tetrahydroimidazo[1,2-a]pyrazin-3-yl)imidazo[1,2-a]pyridine-3-carboxamideHCID 5326209026.3%

反応条件

温度140 °C

反応手順

7-Bromo-N-(3-ethyl-1-((6-methylpyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide (prepared as in Example 127, Step A; 50 mg, 0.10 mmol) in DMF (4 mL) was added tert-butyl 5,6-dihydroimidazo[1,2-a]pyrazine-7(8H)-carboxylate (68 mg, 0.31 mmol), Pd(PPh3)4 (12 mg, 0.01 mmol), palladium diacetate (2.3 mg, 0.010 mmol) and K2CO3 (42 mg, 0.31 mmol). The reaction mixture was purged with argon and the reaction vial was sealed and the mixture was heated to 140° C. for 3 hours. The mixture was cooled to ambient temperature and diluted with DCM (20 mL). The solution was washed with H2O, dried (Na2SO4) and concentrated under reduced pressure. The residue was purified by silica gel chromatography (DCM/MeOH/NH4OH 10:1:0.1) to provide the final product (14 mg). MS (ES+APCI) m/z=532 (M+H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08841455B2
出典データセットuspto-grants-2014_09
ORD IDord-50c00976280348d0b5e801d60b2b650b
出典メモuspto-grants-2014_09