Donepezil → Donepezil Maleate

HRID 1888057Notes

Reaction equation

HRID 1888057 reaction equation
[C:1]([OH:8])(=[O:7])/[CH:2]=[CH:3]\[C:4]([OH:6])=[O:5].[CH3:9][O:10][C:11]1[CH:12]=[C:13]2[CH2:22][CH:21]([CH2:23][CH:24]3[CH2:29][CH2:28][N:27]([CH2:30][C:31]4[CH:32]=[CH:33][CH:34]=[CH:35][CH:36]=4)[CH2:26][CH2:25]3)[C:19](=[O:20])[C:14]2=[CH:15][C:16]=1[O:17][CH3:18]>C(OCC)(=O)C>[CH3:9][O:10][C:11]1[CH:12]=[C:13]2[CH2:22][CH:21]([CH2:23][CH:24]3[CH2:25][CH2:26][N:27]([CH2:30][C:31]4[CH:36]=[CH:35][CH:34]=[CH:33][CH:32]=4)[CH2:28][CH2:29]3)[C:19](=[O:20])[C:14]2=[CH:15][C:16]=1[O:17][CH3:18].[C:1]([O-:8])(=[O:7])/[CH:2]=[CH:3]\[C:4]([O-:6])=[O:5]

Participants

4

Reactant 2

HCID 3152DonepezilHCID 444266Maleic Acid

Product 1

HCID 24801486Donepezil Maleate

Reagents, catalysts & solvents 1

HCID 8857Ethyl AcetateSolvent

Procedure

Maleic acid (1.161 g, dissolved in 35 ml of acetone) is slowly added to a solution of Donepezil (3.79 g) in ethyl acetate (70 ml) with stirring at room temperature. The mixture is stirred for 3 hours at room temperature and concentrated at vacuum to give the title compound.

Workup

  1. stirringThe mixture is stirred for 3 hours at room temperature
  2. concentrationconcentrated at vacuum

Sources & evidence

ORD record
ord-dc5f57ac8e2f45fbb166922a6966e02b
Source dataset
uspto-grants-2013_08
Patent number
US08501779B2

Reaction notes

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