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HRID 448575作成日:2026年10月25日

Water → 1-(4-Chloro-[1,3,5]-triazin-2-yl)-5-methanesulfonyl-2,3-dihydro-1H-indole

https://huagongshe.com/reaction/448575

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Cesium carbonateHCID 10796—
反応物2,4-Dichloro-1,3,5-triazineHCID 17810—
反応物5-(Methanesulfonyl)-2,3-dihydro-1H-indoleHCID 2736136—
触媒palladium(II) acetateHCID 167845—
触媒Binap, (A+-)-HCID 634876—
溶媒1,4-DioxaneHCID 31275—
生成物1-(4-Chloro-[1,3,5]-triazin-2-yl)-5-methanesulfonyl-2,3-dihydro-1H-indoleHCID 8665017583.7%

反応条件

温度100 °C

反応手順

5-Methanesulfonyl-2,3-dihydro-1H-indole (79 mg, 0.4 mmol) was dissolved in dioxane (2 mL). 2,4-Dichloro-[1,3,5]-triazine (60 mg, 1 eq), palladium acetate (11 mg, 5% molar), (+/−)binap (15 mg, 8% molar) and cesium carbonate (131 mg, 1 eq) were added and the reaction mixture was heated at 100° C. for 4 h. The mixture was cooled to room temperature and water was added. The mixture was filtered through celite and washed three times with dioxane. The collected filtrate was evaporated to dryness to give 11a (104 mg) which was used for the next step without further purification.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08481731B2
出典データセットuspto-grants-2013_07
ORD IDord-c6be3730c18143329c854589768305da
出典メモuspto-grants-2013_07