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Triethylamine → (2R*,4S*)-2-benzyl-1-(3,5-bis(trifluoromethyl)benzoyl)-N-(2-phenylethyl)-N-trifluoroacetyl-4-piperidinamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 3,5-Bis(trifluoromethyl)benzoic acid | HCID 12889 | — |
| 反応物 | Bis(2-oxo-3-oxazolidinyl)phosphinic chloride | HCID 152842 | — |
| 反応物 | (2R*,4S*)-2-Benzyl-N-(2-phenylethyl)-N-trifluoroacetyl-4-piperidinamine | HCID 22863105 | — |
| 生成物 | (2R*,4S*)-2-benzyl-1-(3,5-bis(trifluoromethyl)benzoyl)-N-(2-phenylethyl)-N-trifluoroacetyl-4-piperidinamine | HCID 57308278 | 79% |
反応手順
150 mg (0.384 mmol) of (2R*,4S*)-2-benzyl-N-(2-phenylethyl)-N-trifluoroacetyl-4-piperidinamine are reacted in analogy to Example 4a with 93 mg (0.461 mmol) of 3,5-bis(trifluoromethyl)benzoic acid, 117 mg (0.461 mmol) of bis(2-oxo-3-oxazolidinyl)phosphinic chloride and 118 μl (0.845 mmol) of triethylamine. The title compound (191 mg, 79%) is obtained as oil. TLC: methylene chloride/methanol/conc. ammonia (2000:50:1) Rf =0.79, FD-MS: M+ =630.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05310743 |
| 出典データセット | uspto-grants-1994_05 |
| ORD ID | ord-3d0da9e2eca94c6aafafc7bf2dd00cad |
| 出典メモ | uspto-grants-1994_05 |