Hydrochloric Acid → Donepezil Hydrochloride

HRID 1602844Notes

Reaction equation

HRID 1602844 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]>>[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

3

Reactant 2

HCID 313Hydrochloric AcidHCID 3152Donepezil

Product 1

HCID 5741Donepezil HydrochlorideYield 96.7%

Conditions

Temperature
22 °C

Procedure

1.0 g of Donepezil was dissolved in the mixture comprising from 0.31 g of concentrated hydrochloric acid and 4 ml of ion exchange purified water under stirring at 22° C. 100 ml of THF was added hereinto. It continued stirring for 30 minutes at room temperature. Filtration of the separated crystals followed by drying afforded 1.06 g of the title compound. (water content: 11.14%)

Workup

  1. custompurified water
  2. addition100 ml of THF was added hereinto
  3. stirringIt continued stirring for 30 minutes at room temperature
  4. filtrationFiltration of the separated crystals
  5. customby drying

Sources & evidence

ORD record
ord-b1b1f58d082345d590b7c72baa367f4c
Source dataset
uspto-grants-1999_11
Patent number
US05985864

Reaction notes

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