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4-(4-Bromo-2-fluorobenzyl)-5-n-butyl-2-(2-chloro-5-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one → 5-n-Butyl-4-[[2'-(N-t-butylsulfamoyl)-3-fluoro-5'-n-propylbiphenyl-4-yl]methyl]-2-(2-chloro-5-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-(4-Bromo-2-fluorobenzyl)-5-n-butyl-2-(2-chloro-5-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one | HCID 19939472 | — |
| 反応物 | (2-(N-(tert-Butyl)sulfamoyl)-5-propylphenyl)boronic acid | HCID 19939476 | — |
| 生成物 | 5-n-Butyl-4-[[2'-(N-t-butylsulfamoyl)-3-fluoro-5'-n-propylbiphenyl-4-yl]methyl]-2-(2-chloro-5-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one | HCID 19939390 | 43% |
反応手順
Using the method of Example 76, Step F, 4-(4-bromo-2-fluorobenzyl)-5-n-butyl-2-(2-chloro-5-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (from Step A) was coupled with 2-(N-t-butylsulfamoyl)-5-n-propylphenylboronic acid (from Example 68, Step B). Flash chromatography of the crude product on silica gel (gradient elution with 6:1 to 2:1 hexane-EtOAc) gave a 43% yield of the title compound as a cream-colored solid, mp 84°-86° C.; homogeneous by TLC (4:1 hexane-EtOAc).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05411980 |
| 出典データセット | uspto-grants-1995_05 |
| ORD ID | ord-c1502034cc6a49d49b7d12eb09a6140b |
| 出典メモ | uspto-grants-1995_05 |