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2-Naphthoic acid → (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-N-(2-naphthoyl)-4-piperidinamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Naphthoic acid | HCID 7123 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Thionyl Chloride | HCID 24386 | — |
| 反応物 | (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-4-piperidinamine | HCID 53839030 | — |
| 生成物 | (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-N-(2-naphthoyl)-4-piperidinamine | HCID 57245764 | 96% |
反応手順
142 mg (0.825 mmol) of 2-naphthoic acid are reacted in analogy to Example 2a first with 2 ml (27 mmol) of thionyl chloride and subsequently with 200 mg (0.550 mmol) of (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-4-piperidinamine and 138 μl (0.991 mmol) of triethylamine to give the title compound (272 mg, 96%). ##STR83## TLC:methylene chloride/methanol/cone. ammonia (1000:50:1) Rf =0.73, FD-MS: (M+H)+ =516, 518, 520, IR:3420, 1625 cm-1.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05646144 |
| 出典データセット | uspto-grants-1997_07 |
| ORD ID | ord-4b309cf9dafc4f0aaa924845a93047e9 |
| 出典メモ | uspto-grants-1997_07 |