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HRID 605963作成日:2026年10月26日

Sodium Carbonate → 4-(8-(4-(4-Isopropylpiperazin-1-yl)phenylamino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-2-carboxamide

https://huagongshe.com/reaction/605963

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物4-{8-[4-(4-Methyl-piperazin-1-yl)-phenylamino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl}-thiophene-2-carboxylic acid amideHCID 57589928—
反応物4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)furan-2-carboxamideHCID 57589990—
反応物(5-Bromo-[1,2,4]triazolo[1,5-a]pyrazin-8-yl)-[6-(4-isopropylpiperazin-1-yl)pyridin-3-yl]amineHCID 57590080—
触媒HCID 178418397HCID 178418397—
溶媒1,4-DioxaneHCID 31275—
生成物4-(8-(4-(4-Isopropylpiperazin-1-yl)phenylamino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-2-carboxamideHCID 23624295—

反応手順

This compound may be prepared using methods as described for Compound 6, step 4, using 5-bromo-N-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-[1,2,4]triazolo[1,5-a]pyrazin-8-amine (80 mg, 0.21 mmol), 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-furan-2-carboxylic acid amide (101 mg, 0.42 mmol), and Pd(PPh3)4 (62 mg, 0.053 mmol) in 1.5M Na2CO3 (aq) (1.143 mL, 1.71 mmol), and dioxane (4 mL). The crude product is purified by silica gel column chromatography eluting with DCM and 97:3 DCM:NH3 (7M in MeOH). The title compound is isolated after trituration with diethyl ether (35.4 mg, 42%). Conversion into the mesylate salt using 1M methanesulfonic acid in MeOH (0.0793 mL) affords the title compound as a solid (35 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07915256B2
出典データセットuspto-grants-2011_03
ORD IDord-a8728b33aed94b09a39d36f9e21449a5
出典メモuspto-grants-2011_03