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3-[(R*)-1-((S)-5-benzyloxy-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-piperidin-3-yl]-phenol → (S)-2-[(R*)-3-(3-Hydroxy-phenyl)-piperidin-1-ylmethyl]-2,3-dihydro-benzo[1,4]dioxin-5-ol

HRID 2407332
Notes
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Reaction equation

HRID 2407332 reaction equation
C([O:8][C:9]1[C:18]2[O:17][CH2:16][C@H:15]([CH2:19][N:20]3[CH2:25][CH2:24][CH2:23][C@H:22]([C:26]4[CH:27]=[C:28]([OH:32])[CH:29]=[CH:30][CH:31]=4)[CH2:21]3)[O:14][C:13]=2[CH:12]=[CH:11][CH:10]=1)C1C=CC=CC=1>C(OCC)(=O)C.[Pd]>[OH:32][C:28]1[CH:27]=[C:26]([C@H:22]2[CH2:23][CH2:24][CH2:25][N:20]([CH2:19][C@@H:15]3[O:14][C:13]4[CH:12]=[CH:11][CH:10]=[C:9]([OH:8])[C:18]=4[O:17][CH2:16]3)[CH2:21]2)[CH:31]=[CH:30][CH:29]=1
ParticipantsProcedureWorkupSources & evidenceReaction notes

Participants

4

Reactant 1

HCID 684875373-[(R*)-1-((S)-5-benzyloxy-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-piperidin-3-yl]-phenol

Product 1

HCID 68486843(S)-2-[(R*)-3-(3-Hydroxy-phenyl)-piperidin-1-ylmethyl]-2,3-dihydro-benzo[1,4]dioxin-5-olYield 100.2%

Reagents, catalysts & solvents 2

HCID 23938PalladiumCatalystHCID 8857Ethyl AcetateSolvent

Procedure

A mixture of 3-[(R*)-1-((S)-5-benzyloxy-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-piperidin-3-yl]-phenol (84 mg, 0.19 mmol) and palladium-on-carbon (60 mg) in ethyl acetate (10 ml) were stirred and hydrogenated for 6 h. The reaction mixture was filtered and washed with ethyl acetate (10 ml), and evaporated to dryness. The crude product was purified with flash chromatography using dichloromethane and methanol as eluents to give 65 mg of the title compound.

Workup

  1. filtrationThe reaction mixture was filtered
  2. washwashed with ethyl acetate (10 ml)
  3. customevaporated to dryness
  4. customThe crude product was purified with flash chromatography

Sources & evidence

ORD record
ord-b107bd21a2664fb28e3f1a3697ff4079
Source dataset
uspto-grants-2014_08
DOI
10.6084/m9.figshare.5104873.v1
Patent number
US08809536B2

Reaction notes

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On this pageParticipantsProcedureWorkupSources & evidenceReaction notes