Hydrochloric Acid → Erlotinib Hydrochloride

HRID 1184630Notes

Reaction equation

HRID 1184630 reaction equation
[CH3:1][O:2][CH2:3][CH2:4][O:5][C:6]1[CH:7]=[C:8]2[C:20]([NH:21][C:22]3[CH:23]=[CH:24][CH:25]=[C:26]([C:28]#[CH:29])[CH:27]=3)=[N:19][CH:18]=[N:17][C:9]2=[CH:10][C:11]=1[O:12][CH2:13][CH2:14][O:15][CH3:16].[ClH:30]>C(OC(C)C)(=O)C>[CH3:1][O:2][CH2:3][CH2:4][O:5][C:6]1[CH:7]=[C:8]2[C:20]([NH:21][C:22]3[CH:23]=[CH:24][CH:25]=[C:26]([C:28]#[CH:29])[CH:27]=3)=[N:19][CH:18]=[N:17][C:9]2=[CH:10][C:11]=1[O:12][CH2:13][CH2:14][O:15][CH3:16].[ClH:30]

Participants

4

Reactant 2

HCID 313Hydrochloric AcidHCID 176870Erlotinib

Product 1

HCID 176871Erlotinib Hydrochloride

Reagents, catalysts & solvents 1

HCID 7915Isopropyl AcetateSolvent

Procedure

The process of the invention may also be carried out by dissolving erlotinib free base in isopropyl acetate to form a clear solution; adding hydrochloric acid to the solution; 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 from the solution.

Workup

  1. customto form a clear solution

Sources & evidence

ORD record
ord-e72c50456127487fad73508f82456955
Source dataset
uspto-grants-2014_03
Patent number
US08669265B2

Reaction notes

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