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HRID 1766253作成日:2026年10月27日

3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol → 2,4-Difluorobenzenesulfonic acid 3-(1-methylpiperidin-4-yl)-1H-indol-5-yl ester

https://huagongshe.com/reaction/1766253

反応式

関与物質

役割名称HCID仕込み量
反応物3-(1-Methyl-4-piperidinyl)-1H-indol-5-olHCID 2438—
反応物Sodium HydroxideHCID 14798—
反応物2,4-Difluorobenzenesulfonyl ChlorideHCID 2734273—
溶媒TetrahydrofuranHCID 8028—
生成物2,4-Difluorobenzenesulfonic acid 3-(1-methylpiperidin-4-yl)-1H-indol-5-yl esterHCID 10294752100.5%

反応手順

By a method similar to Example 31, using 2,4-difluorobenzenesulfonyl chloride (463 mg, 2.2 mmol) was added to a solution of 3-(1-methylpiperidin-4-yl)-5-hydroxy-1H-indole (418 mg, 1.8 mmol) in 0.2 N sodium hydroxide (10 mL, 2.0 mmol) and THF (5 mL) gave 735 mg of product. The crude product was recrystallized from ethyl acetate/hexanes to give 680 mg (92%) of white crystals: mp=163-164° C.; MS(m/e): 406 (M+); Calculated for C20H20F2N2O3S: C, 59.10; H, 4.96; N, 6.89. Found: C, 58.86; H, 4.94; N, 6.95.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07230011B2
出典データセットuspto-grants-2007_06
ORD IDord-3263906d8e394de4afb2f1f453bfbc69
出典メモuspto-grants-2007_06