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HRID 25411作成日:2026年10月26日

Sodium Bicarbonate → 2-methylsulfonyl-N-(3-thiophen-3-yl-1H-indazol-5-yl)benzenesulfonamide

https://huagongshe.com/reaction/25411

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium BicarbonateHCID 516892—
反応物Thiophene-3-boronic acidHCID 581760—
反応物tert-butyl 3-iodo-5-(N-tert-butoxycarbonyl-2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylateHCID 22567083—
溶媒DimethylformamideHCID 6228—
生成物2-methylsulfonyl-N-(3-thiophen-3-yl-1H-indazol-5-yl)benzenesulfonamideHCID 2256737716.9%

反応手順

2-Methylsulfonyl-N-(3-thiophen-3-yl-1H-indazol-5-yl)benzenesulfonamide can be obtained as described in Example 47 from 1 g of tert-butyl 3-iodo-5-(N-tert-butoxycarbonyl-2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylate, 376 mg of 3-thiopheneboronic acid, 40 ml of dimethylformamide, 3.2 ml of a saturated aqueous sodium hydrogencarbonate solution and 42.7 mg of tetrakis(triphenylphosphine)palladium[0]. 108 mg of 2-methylsulfonyl-N-(3-thiophen-3-yl-1H-indazol-5-yl)benzenesulfonamide are thus obtained in the form of a white solid melting at 249° C. (analysis C18H15N3O4S3 % calculated C, 49.87; H, 3.49; N, 9.69; O, 14.76; S, 22.19. % found C, 49.76; H, 3.53; N, 10.03; S, 21.78).

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-b009021cfef944529dd20582858ec702
出典メモuspto-grants-2005_02