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Triethylamine → 1-(6,7-Dibutoxy-2-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine hydrochloride
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Diethyl cyanophosphonate | HCID 76257 | — |
| 反応物 | 1-[(3,4,5-Trimethoxyphenyl)methyl]piperazine;dihydrochloride | HCID 12828501 | — |
| 反応物 | 6,7-Dibutoxy-2-naphthoic acid | HCID 14676193 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 1-(6,7-Dibutoxy-2-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine hydrochloride | HCID 19841242 | 84.2% |
反応手順
Using 6,7-dibutoxy-2-naphthoic acid (0.25 g), 1-(3,4,5-trimethoxybenzyl)piperazine dihydrochloride (0.31 g), triethylamine (0.35 g), N,N-dimethylformamide (10 ml) and diethyl phosphorocyanidate (0.5 ml), an amidation as that described in Example 6 is carried out. The reaction mixture is purified by gel column chromatography (hexane:acetone=1:1) and converted to the hydrochloride in ethyl acetate to give 1-(6,7-dibutoxy-2-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine hydrochloride (0.4 g) as colorless prisms, m.p. 182°-185° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04880809 |
| 出典データセット | uspto-grants-1989_11 |
| ORD ID | ord-10f32baff4434981a2195c42437e77cb |
| 出典メモ | uspto-grants-1989_11 |