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Isoquinoline, 1-chloro- → [1-(1-Isoquinolyl)-4-piperidyl]methanol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Isoquinoline, 1-chloro- | HCID 140539 | — |
| 反応物 | 4-Piperidinemethanol | HCID 420771 | — |
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | Sodium t-butoxide | HCID 23676156 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 生成物 | [1-(1-Isoquinolyl)-4-piperidyl]methanol | HCID 21096912 | — |
反応手順
The process is performed as described in Example 2 (step 2.1). Starting with 2.50 g (15.28 mmol) of 1-chloroisoquinoline, 1.94 g (136.6 mmol) of 4-piperidylmethanol, 3.53 g (36.67 mmol) of sodium tert-butoxide, 0.285 g (0.46 mmol) of BINAP and 0.140 g (0.15 mmol) of tris(dibenzylideneacetone)dipalladium, and after chromatography on silica gel, eluting with a 98/2/0.2 and then 95/5/0.5 mixture of dichloromethane, methanol and 28% aqueous ammonia, 2.40 g of pure product are obtained in the form of a viscous orange oil.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08034818B2 |
| 出典データセット | uspto-grants-2011_10 |
| ORD ID | ord-922d58f6a38145bca556ab8248623dfd |
| 出典メモ | uspto-grants-2011_10 |