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Binap, (A+-)- → N-[4-Chloro-2(pyridine-4-carbonyl)-phenyl]-4-(1,1-dioxo-thiomorpholin-4-yl)-benzenesulfonamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | Thiomorpholine 1,1-dioxide | HCID 6484228 | — |
| 反応物 | 4-Bromo-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamide | HCID 10072530 | — |
| 反応物 | Potassium phosphate, tribasic, monohydrate | HCID 22031701 | — |
| 触媒 | Palladium | HCID 23938 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | N-[4-Chloro-2(pyridine-4-carbonyl)-phenyl]-4-(1,1-dioxo-thiomorpholin-4-yl)-benzenesulfonamide | HCID 59788575 | — |
反応手順
The title compound was prepared according to the general procedure for the synthesis of heterocyclyl and heteroaryl substituted phenylsulfonyl derivatives previously described, using 4-Bromo-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamide 0.3 g (0.66 mmol), potassium phosphate tribasic monohydrate 0.91 g (3.96 mmol), rac-2,2′-bis (diphenylphosphino)-1,1′-binaphthyl 0.12 g (0.198 mmol), thiomorpholine 1,1-dioxide 0.44 g (3.3 mmol) and Pd (dba)3 60 mg (0.066 mmol) in 6 ml dioxane, followed by work up and HPLC purification: LC-MSD, m/z for C22H20ClN3O3S2 [M+H]+: 502
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07420055B2 |
| 出典データセット | uspto-grants-2008_09 |
| ORD ID | ord-bc22d2ac57ca47c6b71cce111ebcf138 |
| 出典メモ | uspto-grants-2008_09 |