Hydrochloric Acid → Donepezil Hydrochloride

HRID 1602836Notes

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]>CN(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

Conditions

Temperature: 40 °C

Procedure

1.0 g of Donepezil was dissolved in 4 ml of DMF under heating at 40° C. The solution was cooled in an iced water bath. 0.31 g of Concentrated hydrochloric acid in 1 ml of DMF was added hereinto. It continued stirring for 30 minutes in an iced water bath. Filtration of the separated crystals followed by drying afforded 1.08 g of the title compound. (water content: 0.72%)

Workup

temperatureThe solution was cooled in an iced water bath
filtrationFiltration of the separated crystals
customby drying

Sources & evidence

ORD record: ord-abf639e3eb2642d8906023efd0d6e40e
Source dataset: uspto-grants-1999_11
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US05985864

Reaction notes

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