Morpholine → 1,1-Dimethylethyl 4-hydroxy-4-(4-morpholinylmethyl)-1-piperidinecarboxylate

HRID 253025ノート

反応式

HRID 253025 の反応式
[C:1]([O:5][C:6]([N:8]1[CH2:15][CH2:14][C:11]2([O:13][CH2:12]2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[NH:16]1[CH2:21][CH2:20][O:19][CH2:18][CH2:17]1>CCO>[C:1]([O:5][C:6]([N:8]1[CH2:15][CH2:14][C:11]([OH:13])([CH2:12][N:16]2[CH2:21][CH2:20][O:19][CH2:18][CH2:17]2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2]

参加物

4

反応物 2

HCID 8083MorpholineHCID 22135564tert-Butyl 1-oxa-6-azaspiro(2.5)octane-6-carboxylate

生成物 1

HCID 583931721,1-Dimethylethyl 4-hydroxy-4-(4-morpholinylmethyl)-1-piperidinecarboxylate収率 67%

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

1-Oxa-6-aza-spiro[2.5]octane-6-carboxylic acid tert-butyl ester (100 mg, 0.47 mmol) and morpholine (42 μL, 0.48 mmol, 1.03 eq) were stirred in EtOH at RT overnight. Solvent was removed in vacuo and the residue purified by flash chromatography (silica gel, 4% MeOH/DCM) to give 4-hydroxy-4-morpholin-4-ylmethyl-piperidine-1-carboxylic acid tert-butyl ester as a white solid (91.4 mg, 67%).

後処理

  1. customSolvent was removed in vacuo
  2. customthe residue purified by flash chromatography (silica gel, 4% MeOH/DCM)

出典と根拠

ORDレコード
ord-1e21c89e02ed47edbf2f4bdbe6a94fec
出典データセット
uspto-grants-2011_01
特許番号
US07872003B2

反応ノート

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