Levofloxacin → Levofloxacin monohydrate

HRID 1077997Notes

Reaction equation

HRID 1077997 reaction equation
[F:1][C:2]1[C:3]([N:20]2[CH2:25][CH2:24][N:23]([CH3:26])[CH2:22][CH2:21]2)=[C:4]2[O:9][CH2:8][C@H:7]([CH3:10])[N:6]3[CH:11]=[C:12]([C:17]([OH:19])=[O:18])[C:13](=[O:16])[C:14]([CH:15]=1)=[C:5]23>O>[OH2:9].[F:1][C:2]1[C:3]([N:20]2[CH2:21][CH2:22][N:23]([CH3:26])[CH2:24][CH2:25]2)=[C:4]2[O:9][CH2:8][C@H:7]([CH3:10])[N:6]3[CH:11]=[C:12]([C:17]([OH:19])=[O:18])[C:13](=[O:16])[C:14]([CH:15]=1)=[C:5]23

Participants

3

Reactant 1

HCID 149096Levofloxacin

Product 1

HCID 178438Levofloxacin monohydrate

Reagents, catalysts & solvents 1

HCID 962WaterSolvent2×

Procedure

A further aspect of the present invention comprises treating (S)-9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]-benzoxazine-6-carboxylic acid in an aqueous solvent of relatively high water content or water to produce (S)-9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid monohydrate. Here, the solvent has a water content which substantially prevents hemihydrate formation. The aqueous solvent is preferably aqueous ethanol.

Sources & evidence

ORD record
ord-9cebff791496467bb1d811a39e34e371
Source dataset
uspto-grants-1996_08
Patent number
US05545737

Reaction notes

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