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2,2-Dimethylsuccinic anhydride → 4-(4-{5-[(1-Ethyl-4-isobutoxy-1H-indole-2-carbonyl)-amino]-pyridin-2-yl}-piperazin-1-yl)-2,2-dimethyl-4-oxo-butyric acid hydrochloric acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2,2-Dimethylsuccinic anhydride | HCID 87067 | — |
| 反応物 | 4-(4-{5-[(4-Chloro-benzo[b]thiophene-2-carbonyl)-amino]-pyridin-2-yl}-piperazin-1-yl)-2,2-dimethyl-4-oxo-butyric acid | HCID 46207828 | — |
| 反応物 | 1-ethyl-4-isobutoxy-1H-indole-2-carboxylic acid (6-piperazin-1-yl-pyridin-3-yl)-amide | HCID 59365189 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 4-(4-{5-[(1-Ethyl-4-isobutoxy-1H-indole-2-carbonyl)-amino]-pyridin-2-yl}-piperazin-1-yl)-2,2-dimethyl-4-oxo-butyric acid hydrochloric acid | HCID 66772454 | — |
反応手順
With a method similar to that used for the preparation of 4-(4-{5-[(4-chloro-benzo[b]thiophene-2-carbonyl)-amino]-pyridin-2-yl}-piperazin-1-yl)-2,2-dimethyl-4-oxo-butyric acid, 4-(4-{5-[(1-ethyl-4-isobutoxy-1,1-indole-2-carbonyl)-amino]-pyridin-2-yl}-piperazin-1-yl)-2,2-dimethyl-4-oxo-butyric acid was prepared from 1-ethyl-4-isobutoxy-1H-indole-2-carboxylic acid (6-piperazin-1-yl-pyridin-3-yl)-amide and 2,2-dimethylsuccinic anhydride. The desired product was dissolved in methylene chloride and treated with gaseous hydrogen chloride in ether. After the evaporation of solvents, a hydrochloride salt was obtained. LCMS for C30H39N5O5 calcd. (m/e) 549, observed 550 (M+H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08124766B2 |
| 出典データセット | uspto-grants-2012_02 |
| ORD ID | ord-e0e12249dc0f40d980889c19ecf9d91c |
| 出典メモ | uspto-grants-2012_02 |