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HRID 1366151作成日:2026年10月26日

1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) → (5-Bromo-imidazo[1,2-a]pyrazin-8-yl)-[4-(4-pyridin-2-yl-[1,2,3]triazol-1-yl)-phenyl]amine

https://huagongshe.com/reaction/1366151

反応式

関与物質

役割名称HCID仕込み量
反応物1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
反応物Sodium t-butoxideHCID 23676156—
反応物N-(4-Hydroxybenzyl)-4-[5-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-ylamino]benzamideHCID 24857547—
反応物5,8-Dibromoimidazo[1,2-a]pyrazineHCID 53485949—
反応物4-(4-Pyridin-2-yl-[1,2,3]triazol-1-yl)-phenylamineHCID 59023133—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
生成物(5-Bromo-imidazo[1,2-a]pyrazin-8-yl)-[4-(4-pyridin-2-yl-[1,2,3]triazol-1-yl)-phenyl]amineHCID 59023107—

反応手順

In the same way as described for Compound 90, step 1, using 5,8-dibromoimidazo[1,2-a]pyrazine (80.5 mg, 0.291 mmol), 4-(4-pyridin-2-yl-[1,2,3]triazol-1-yl)-phenylamine (68.3 g, 0.288 mmol), NaOtBu (38.2 mg, 0.403 mmol), Pd2(dba)3 (10.5 mg, 0.0115 mmol), Xantphos (13.3 mg, 0.023mmol) and toluene (4 mL). The crude material is purified by silica gel column chromatography eluting with 98:2 DCM:MeOH followed by 97:3 DCM:MeOH affording the title compound (52.8 mg, 42%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07893058B2
出典データセットuspto-grants-2011_02
ORD IDord-cf5af2bf34b34aa8992337fb51c4d67b
出典メモuspto-grants-2011_02