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Sodium Bicarbonate → N-[3-(1H-indol-2-yl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium Bicarbonate | HCID 516892 | — |
| 反応物 | 1-(tert-Butoxycarbonyl)indole-2-boronic Acid (contains varying amounts of Anhydride) | HCID 2773302 | — |
| 反応物 | Tert-butyl 3-iodo-5-(2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylate | HCID 22567134 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-[3-(1H-indol-2-yl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamide | HCID 135621937 | 40.8% |
反応手順
N-[3-(1H-Indol-2-yl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamide can be obtained as described in Example 59 from 1 g of tert-butyl 3-iodo-5-(2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylate, 900 mg 1-(tert-butyloxycarbonyl)indole-2-boronic acid, 40 ml of dimethylformamide, 3.2 ml of saturated aqueous sodium hydrogencarbonate solution and 50 mg of tetrakis(triphenylphosphine)palladium[0]. 330 mg of N-[3-(1H-indol-2-yl)-1H-indazol-5-yl]-2-methylsulfonylbenzenesulfonamide are thus obtained in the form of a white solid melting above 260° C. (analysis C22H18N4O4S2 % calculated C, 56.63; H, 3.89; N, 12.01; O, 13.72; S, 13.75. % found C, 56.87; H, 4.10; N, 13.81; S, 12.65).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06858638B2 |
| 出典データセット | uspto-grants-2005_02 |
| ORD ID | ord-7de1cfd29f2947ffa34048b2d104d656 |
| 出典メモ | uspto-grants-2005_02 |