Diisopropylethylamine → Ethyl-2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-oxazole-4-carboxylate

HRID 561239ノート

反応式

HRID 561239 の反応式
[Br:1][C:2]1[CH:14]=[CH:13][C:12]([F:15])=[CH:11][C:3]=1[O:4][CH:5]1[CH2:10][CH2:9][NH:8][CH2:7][CH2:6]1.Cl[C:17]1[O:18][CH:19]=[C:20]([C:22]([O:24][CH2:25][CH3:26])=[O:23])[N:21]=1.CCN(C(C)C)C(C)C>CCO>[CH2:25]([O:24][C:22]([C:20]1[N:21]=[C:17]([N:8]2[CH2:7][CH2:6][CH:5]([O:4][C:3]3[CH:11]=[C:12]([F:15])[CH:13]=[CH:14][C:2]=3[Br:1])[CH2:10][CH2:9]2)[O:18][CH:19]=1)=[O:23])[CH3:26]

参加物

5

反応物 3

HCID 81531DiisopropylethylamineHCID 2763184Ethyl 2-chlorooxazole-4-carboxylateHCID 578327574-(2-Bromo-5-fluorophenoxy)piperidine

生成物 1

HCID 66696829Ethyl-2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-oxazole-4-carboxylate

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

To a solution of 4-(2-bromo-5-fluorophenoxy)piperidine (3.281 g, 11.97 mmol) in EtOH (28.5 mL) was added ethyl 2-chlorooxazole-4-carboxylate (1 g, 5.70 mmol) and DIPEA (1.990 mL, 11.39 mmol). The reaction mixture was stirred at rt for 5 h. The solvent was evaporated under reduced pressure. The residue was diluted with 1N HCl and extracted with EtOAc. The combined organic layers were dried (MgSO4), filtered and evaporated under reduced pressure to give the title compound.

後処理

  1. customThe solvent was evaporated under reduced pressure
  2. additionThe residue was diluted with 1N HCl
  3. extractionextracted with EtOAc
  4. dry with materialThe combined organic layers were dried (MgSO4)
  5. filtrationfiltered
  6. customevaporated under reduced pressure

出典と根拠

ORDレコード
ord-38931cb3ba214a42945869ec5193b004
出典データセット
uspto-grants-2011_11
特許番号
US08063224B2

反応ノート

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