Hydrochloric Acid → Donepezil Hydrochloride

HRID 1602842Notes

Reaction equation

HRID 1602842 reaction equation
[CH3:1][O:2][C:3]1[CH:4]=[C:5]2[CH2:14][CH:13]([CH2:15][CH:16]3[CH2:21][CH2:20][N:19]([CH2:22][C:23]4[CH:24]=[CH:25][CH:26]=[CH:27][CH:28]=4)[CH2:18][CH2:17]3)[C:11](=[O:12])[C:6]2=[CH:7][C:8]=1[O:9][CH3:10].[ClH:29].C(OC(C)C)(C)C>C(O)C>[CH3:1][O:2][C:3]1[CH:4]=[C:5]2[CH2:14][CH:13]([CH2:15][CH:16]3[CH2:17][CH2:18][N:19]([CH2:22][C:23]4[CH:28]=[CH:27][CH:26]=[CH:25][CH:24]=4)[CH2:20][CH2:21]3)[C:11](=[O:12])[C:6]2=[CH:7][C:8]=1[O:9][CH3:10].[ClH:29]

Participants

5

Reactant 3

HCID 313Hydrochloric AcidHCID 3152DonepezilHCID 7914Diisopropyl Ether

Product 1

HCID 5741Donepezil Hydrochloride

Reagents, catalysts & solvents 1

HCID 702EthanolSolvent

Conditions

Temperature
40 °C

Procedure

10.0 g of Donepezil was dissolved in 100 ml of ethanol under heating at 40° C. The solution was cooled to room temperature. 3.01 g of Concentrated hydrochloric acid was added hereinto at 20° C. inner temperature. The solution was set in an oil bath, and was heated to 40° C. inner temperature. 150 ml of isopropyl ether was added hereinto at 40° C. inner temperature. It continued stirring for 20 minutes at 60° C. inner temperature. Filtration of the separated crystals followed by drying afforded the title compound.

Workup

  1. temperatureThe solution was cooled to room temperature
  2. customThe solution was set in an oil bath
  3. temperaturewas heated to 40° C. inner temperature
  4. filtrationFiltration of the separated crystals
  5. customby drying

Sources & evidence

ORD record
ord-7c03147811d34ea0b6052497f46b0291
Source dataset
uspto-grants-1999_11
Patent number
US05985864

Reaction notes

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