関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 5-Bromopyrimidine | HCID 78344 | — |
| 反応物 | 4-Amino-1-Boc-piperidine | HCID 1268291 | — |
| 反応物 | sodium 2-methylpropan-2-olate | HCID 178418730 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | 4-(Pyrimidin-5-ylamino)-piperidine-1-carboxylic acid tert-butyl ester | HCID 67198211 | 73.1% |
反応手順
A mixture of 5-bromopyrimidine (325 mg, 2.04 mmol), 4-amino-1-Boc-piperidine (425 mg, 2.12 mmol), Pd2(dba)3 (41 mg, 0.045 mmol), (±)-BINAP (78 mg, 0.13 mmol) and t-BuONa (210 mg, 2.19 mmol) in freshly degassed toluene (7.0 mL) was stirred at 85° C. under argon for 2 hours. Basic work-up and purification gave 4-(pyrimidin-5-ylamino)-piperidine-1-carboxylic acid tert-butyl ester as a pale brown solid (415 mg, 73%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07491735B2 |
|---|
| 出典データセット | uspto-grants-2009_02 |
|---|
| ORD ID | ord-81bed1ea779e4b80bfa9bbd0f36a06e6 |
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| 出典メモ | uspto-grants-2009_02 |
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