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HRID 25419作成日:2026年10月26日

3-Aminophenylboronic acid → N-[3-(3-aminophenyl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamide

https://huagongshe.com/reaction/25419

反応式

関与物質

役割名称HCID仕込み量
反応物3-Aminophenylboronic acidHCID 92269—
反応物Sodium BicarbonateHCID 516892—
反応物Tert-butyl 3-iodo-5-(2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylateHCID 22567134—
溶媒DimethylformamideHCID 6228—
生成物N-[3-(3-aminophenyl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamideHCID 2256728826.6%

反応手順

N-[3-(3-Aminophenyl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamide can be obtained as described in Example 59 from 0.5 g of tert-butyl 3-iodo-5-(2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylate, 276 mg of 3-aminophenylboronic acid, 20 ml of dimethylformamide, 1.6 ml of a saturated aqueous sodium hydrogencarbonate solution and 25 mg of tetrakis(triphenylphosphine)palladium[0]. 102 mg of N-[3-(3-aminophenyl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamide are thus obtained in the form of a white solid melting at 220° C. (analysis C20H18N4O4S2 % calculated C, 54.29; H, 4.10; N, 12.66; O, 14.46; S, 14.49. % found C, 53.48; H, 4.11 N, 12.50; S, 13.95).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06858638B2
出典データセットuspto-grants-2005_02
ORD IDord-08dd38ead252469fb9b9f20f1e1920c6
出典メモuspto-grants-2005_02