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Binap, (A+-)- → N-[4-Chloro-2-(6-methyl-pyridine-3-carbonyl)-phenyl]-4-(cis-2,6-dimethyl-morpholin-4-yl)-3-fluoro-benzenesulfonamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | 2,6-Dimethylmorpholine, cis- | HCID 641500 | — |
| 反応物 | Potassium phosphate, tribasic, monohydrate | HCID 22031701 | — |
| 反応物 | 4-Bromo-N-[4-chloro-2-(6-methyl-pyridine-3-carbonyl)-phenyl]-3-fluoro-benzenesulfonamide | HCID 59788573 | — |
| 触媒 | Palladium | HCID 23938 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-[4-Chloro-2-(6-methyl-pyridine-3-carbonyl)-phenyl]-4-(cis-2,6-dimethyl-morpholin-4-yl)-3-fluoro-benzenesulfonamide | HCID 59788542 | — |
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-(6-methyl-pyridine-3-carbonyl)-phenyl]-3-fluoro-benzenesulfonamide 0.2 g (0.4 mmol), potassium phosphate tribasic monohydrate 0.570 g (2.4 mmol), rac-2,2′-bis (diphenylphosphino)-1,1′-binaphthyl 0.077 g (0.12 mmol), cis-2,6-dimethyl-morpholine 0.23 g (2 mmol) and Pd (dba)3 0.057 g (0.06 mmol) in 2 ml DMF. HPLC purification gave yellow compound.
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-5bba3fa6d3cb45bfbb0167fa9013705c |
| 出典メモ | uspto-grants-2008_09 |