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HRID 50073作成日:2026年10月25日
Potassium Carbonate → 3-[3-(4-Amino-4-phenylpiperid-1-yl)propyl]-1-benzoyl-3-(3,4-dichlorophenyl)-piperidine
https://huagongshe.com/reaction/50073
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 1-Benzoyl-3-(3,4-dichlorophenyl)-3-[3-[4-(pyrrolidin-1-ylcarbonyl)piperid-1-yl]propyl]piperidine hydrochloride | HCID 22741714 | — |
| 反応物 | 4-Amino-4-phenylpiperidine dibenzenesulfonate | HCID 22741754 | — |
| 溶媒 | acetonitrile N,N-dimethylformamide | HCID 21891449 | — |
| 生成物 | 3-[3-(4-Amino-4-phenylpiperid-1-yl)propyl]-1-benzoyl-3-(3,4-dichlorophenyl)-piperidine | HCID 15285591 | 74.6% |
反応手順
A mixture of 6.81 g of 4-amino-4-phenylpiperidine dibenzenesulfonate, 5.2 g of the compound obtained in step B of EXAMPLE 1 and 6.1 g of K2CO3 in 30 ml of a DMF/acetonitrile mixture (50/50; v/v) is heated at 100° C. for 5 hours. It is concentrated under vacuum, the residue is taken up with water and extracted with AcOEt, the organic phase is washed with water and with saturated NaCl solution and dried over MgSO4 and the solvent is evaporated off under vacuum. The residue is chromatographed on silica H using a DCM/MeOH mixture (from 99/1; v/v to 85/15; v/v) as the eluent to give 3.6 g of the expected product.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06710042B2 |
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| 出典データセット | uspto-grants-2004_03 |
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| ORD ID | ord-7452e02e40fe423e8265ad2b71445983 |
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| 出典メモ | uspto-grants-2004_03 |
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