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Triethylamine → (2R,4S)-N-[1-(3,5-Bis-trifluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-quinazoline-4-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 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-1-(3,5-bis-(trifluoromethyl)benzoyl)-4-piperidinamine | HCID 22869971 | — |
| 反応物 | Quinazoline-4-carboxylic acid | HCID 23008716 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | (2R,4S)-N-[1-(3,5-Bis-trifluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-quinazoline-4-carboxamide | HCID 18392943 | — |
反応手順
Analogously to Example 1, 252 mg (1.45 mmol) of (2R,4S)-2-benzyl-1-(3,5-bis-trifluoromethyl-benzoyl)-4-piperidineamine in 5 ml of methylene chloride are reacted with 368 mg (1.45 mmol) of bis(2-oxo-3-oxazolidinyl)phosphinic acid chloride, 440 mg (4.35 mmol) of triethylamine and 566 mg (1.32 mmol) of quinazoline-4-carboxylic acid. The title compound is obtained in the form of white crystals. M.p.: 92-172° C.; TLC: hexane/ethyl acetate (1:1) Rf =0.37, FD-MS: M+ =586; [alpha]D=+1.3 (c=0.98, methylene chloride). ##STR16##
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05965562 |
| 出典データセット | uspto-grants-1999_10 |
| ORD ID | ord-80a2adb8846940f9ae3bfcc6e0193f32 |
| 出典メモ | uspto-grants-1999_10 |