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HRID 64作成日:2026年10月23日

3-(2,5-Dichloropyrimidin-4-yl)imidazo[1,2-a]pyridine → N-(4-(azetidin-3-yloxy)-2-methoxyphenyl)-5-chloro-4-(imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-amine

https://huagongshe.com/ja/reaction/64

反応式

関与物質

役割名称HCID仕込み量
反応物3-(2,5-Dichloropyrimidin-4-yl)imidazo[1,2-a]pyridineHCID 46934605—
反応物Tert-butyl 3-(4-amino-3-methoxyphenoxy)azetidine-1-carboxylateHCID 59291149—
試薬Cesium carbonateHCID 10796—
触媒1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
触媒Palladium (II) acetateHCID 4144353—
溶媒1,4-DioxaneHCID 31275—
生成物N-(4-(azetidin-3-yloxy)-2-methoxyphenyl)-5-chloro-4-(imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-amineHCID 453815460%

反応条件

温度105 °C

反応手順

3-(2,5-dichloropyrimidin-4-yl)imidazo[1,2-a]pyridine (100 mg, 0.38 mmol) _,_ tert-butyl 3-(4-amino-3-methoxyphenoxy)azetidine-1-carboxylate (111 mg, 0.38 mmol) _,_ CESIUM CARBONATE (246 mg, 0.75 mmol) _,_ diacetoxypalladium (3.39 mg, 0.02 mmol) _and_ 9,9-DIMETHYL-4,5-BIS(DIPHENYLPHOSPHINO)XANTHENE (17.46 mg, 0.03 mmol) ___were_ ___suspended_ _in_ 1,4-dioxane (1 ml) _and degased with argon.The reaction was heated from 60°C to 105°C for 3 hours.Doubt about the LCMS,deprotection of the BOC with TFA to confirm the dialkylation._ No good product

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-297038d2636048ff93bf3571d541a46e
出典メモ750 AstraZeneca ELN dataset