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Acetaldehyde → 4-{[3-(2-Chloro-pyrimidin-4-yl)-benzyl]-ethyl-amino}-piperidine-1-carboxylic acid tert-butyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Acetaldehyde | HCID 177 | — |
| 反応物 | 4-Amino-1-Boc-piperidine | HCID 1268291 | — |
| 反応物 | Sodium triacetoxyborohydride | HCID 5049666 | — |
| 反応物 | 3-(2-Chloro-pyrimidin-4-yl)-benzaldehyde | HCID 24901965 | — |
| 生成物 | 4-{[3-(2-Chloro-pyrimidin-4-yl)-benzyl]-ethyl-amino}-piperidine-1-carboxylic acid tert-butyl ester | HCID 86603290 | — |
反応手順
Intermediate 1 was coupled with 4-Amino-piperidine-1-carboxylic acid tert-butyl ester following procedure B. When the starting aldehyde had been consumed, 2 equivalents each of acetaldehyde and sodium triacetoxyborohydride were added and the mixture stirred for another two hours. The organic layer was washed with water followed by sat. NaCl. The solvent was removed to give product LC-MS showed the product was >90% pure and had the expected M+H+ of 403, and it was used in the following reactions without purification.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07732444B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-0997701628974c5a9df0267362e8f45d |
| 出典メモ | uspto-grants-2010_06 |