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

HRID 253025노트

반응식

HRID 253025 반응식
[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]

참가 물질

4

반응물 2

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

생성물 1

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

시약·촉매·용매 1

HCID 702Ethanol용매

실험 절차

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%).

후처리

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

출처 및 근거

ORD 기록
ord-1e21c89e02ed47edbf2f4bdbe6a94fec
출처 데이터셋
uspto-grants-2011_01
특허 번호
US07872003B2

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