Silica → Diltiazem

HRID 129700Notes

Reaction equation

[CH3:1][C:2]([O:4][C@H:5]1[C:15](=[O:16])[N:14]([CH2:17][CH2:18][N:19]([CH3:21])[CH3:20])[C:13]2[CH:12]=[CH:11][CH:10]=[CH:9][C:8]=2[S:7][C@H:6]1[C:22]1[CH:23]=[CH:24][C:25]([O:28][CH3:29])=[CH:26][CH:27]=1)=[O:3].Cl.C(O)(=O)/C=C/C(O)=O.[Si](=O)=O>>[CH3:1][C:2]([O:4][C@H:5]1[C:15](=[O:16])[N:14]([CH2:17][CH2:18][N:19]([CH3:21])[CH3:20])[C:13]2[CH:12]=[CH:11][CH:10]=[CH:9][C:8]=2[S:7][C@H:6]1[C:22]1[CH:23]=[CH:24][C:25]([O:28][CH3:29])=[CH:26][CH:27]=1)=[O:3]

Participants

Reactant 3

HCID 24261Silica

HCID 62920Diltiazem Hydrochloride2×

HCID 444972Fumaric Acid

Product 1

HCID 39186Diltiazem

Procedure

To an 80 cubic foot blender is charged 188.0 kg of diltiazem HCl, 94.0 kg of fumaric acid NF, 94.0 kg of talc, 2.8 kg of silicon dioxide, and an additional 188.0 kg of diltiazem HCl. The mixture is dry blended for 15 minutes and then milled through a 0.013 inch screen using a conventional milling machine to a sufficiently fine particle size, averaging about 75 microns.

Workup

customThe mixture is dry blended for 15 minutes
custommilled through a 0.013 inch screen

Sources & evidence

ORD record: ord-3dd5b57095734c00b7e84528b23e2ce3
Source dataset: uspto-grants-1995_11
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US05470584

Reaction notes

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