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3,5-Dihydroxybenzoic Acid → (2R*,4S*)-2-benzyl-1-(3,5-dihydroxybenzoyl)-N-(4-quinolylmethyl)-N-trifluoroacetyl-4-piperidinamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3,5-Dihydroxybenzoic Acid | HCID 7424 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Bis(2-oxo-3-oxazolidinyl)phosphinic chloride | HCID 152842 | — |
| 反応物 | (2R*,4S*)-2-Benzyl-N-(4-quinolylmethyl)-N-trifluoroacetyl-4-piperidinamine | HCID 57202094 | — |
| 生成物 | (2R*,4S*)-2-benzyl-1-(3,5-dihydroxybenzoyl)-N-(4-quinolylmethyl)-N-trifluoroacetyl-4-piperidinamine | HCID 56976894 | 38% |
反応手順
200 mg (0.467 mmol) of (2R*,4S*)-2-benzyl-N-(4-quinolylmethyl)-N-trifluoroacetyl-4-piperidinamine are reacted in analogy to Example 4a with 87 mg (0.562 mmol) of 3,5-dihydroxybenzoic acid, 143 mg (0.561 mmol)of bis-(2-oxo-3-oxazolidinyl)phosphinic chloride and 144 μl (1.03 mmol) of triethylamine. The title compound (99 mg, 38%) is obtained as white foam. TLC: methylene chloride/methanol/conc. ammonia (700:50:1) Rf =0.41, FD-MS: M+ =563.
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-34d93cde0e5d4f3d9fd907f5f45f778c |
| 出典メモ | uspto-grants-1997_07 |