Hydrochloric Acid → Erlotinib Hydrochloride

HRID 1184629Notes

Reaction equation

HRID 1184629 reaction equation
[ClH:1].[CH3:2][O:3][CH2:4][CH2:5][O:6][C:7]1[CH:8]=[C:9]2[C:21]([NH:22][C:23]3[CH:24]=[CH:25][CH:26]=[C:27]([C:29]#[CH:30])[CH:28]=3)=[N:20][CH:19]=[N:18][C:10]2=[CH:11][C:12]=1[O:13][CH2:14][CH2:15][O:16][CH3:17]>C(OC(C)C)(=O)C>[CH3:2][O:3][CH2:4][CH2:5][O:6][C:7]1[CH:8]=[C:9]2[C:21]([NH:22][C:23]3[CH:24]=[CH:25][CH:26]=[C:27]([C:29]#[CH:30])[CH:28]=3)=[N:20][CH:19]=[N:18][C:10]2=[CH:11][C:12]=1[O:13][CH2:14][CH2:15][O:16][CH3:17].[ClH:1]

Participants

4

Reactant 2

HCID 313Hydrochloric AcidHCID 176870Erlotinib

Product 1

HCID 176871Erlotinib Hydrochloride

Reagents, catalysts & solvents 1

HCID 7915Isopropyl AcetateSolvent

Procedure

According to another aspect of the present invention, a process is provided for preparation of erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 μm to 15 μm and 90 volume-% of the particles (D90) ranging from about 14 μm to 30 μm, which comprises adding hydrochloric acid to a solution of erlotinib free base in isopropyl acetate, and isolating erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 μm to 15 μm and 90 volume-% of the particles (D90) ranging from about 14 μm to 30 μm.

Sources & evidence

ORD record
ord-ad90b7fadeec4315a50ef360c6f2f3ae
Source dataset
uspto-grants-2014_03
Patent number
US08669265B2

Reaction notes

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