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1-(Bromomethyl)-4-(1,1-dimethylethyl)benzene → 1-(4-(tert-butyl)benzyl)-5-(1H-pyrazol-4-yl)indoline
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-(Bromomethyl)-4-(1,1-dimethylethyl)benzene | HCID 87836 | — |
| 反応物 | 5-Bromoindoline | HCID 3411566 | — |
| 反応物 | tert-butyl 4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-carboxylate | HCID 16217654 | — |
| 反応物 | 1-(4-Isopropylbenzyl)-5-(1H-pyrazol-4-yl)indoline | HCID 90011062 | — |
| 触媒 | Palladium | HCID 23938 | — |
| 生成物 | 1-(4-(tert-butyl)benzyl)-5-(1H-pyrazol-4-yl)indoline | HCID 90068395 | — |
反応手順
1-(4-Isopropylbenzyl)-5-(1H-pyrazol-4-yl)indoline, 50 can be prepared by alkylation of 5-bromoindoline, 22 with 1-(bromomethyl)-4-(tert-butyl)benzene using the conditions described in Example 7, part 1 followed by palladium catalyzed coupling of the alkylation product with tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-carboxylate, 10 followed by hydrolysis using the reaction conditions described in Example 8.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09447069B2 |
| 出典データセット | uspto-grants-2016_09 |
| ORD ID | ord-34a0cdaace674f89aedd0d1f89de34d7 |
| 出典メモ | uspto-grants-2016_09 |