(+)-Lactose → Ketotifen

HRID 1608912Notes

Reaction equation

HRID 1608912 reaction equation
[CH3:1][N:2]1[CH2:22][CH2:21][C:5](=[C:6]2[C:17]3[C:12](=[CH:13][CH:14]=[CH:15][CH:16]=3)[CH2:11][C:9](=[O:10])[C:8]3[S:18][CH:19]=[CH:20][C:7]2=3)[CH2:4][CH2:3]1.C(/C(O)=O)=C\C(O)=O.OC1O[C@H](CO)[C@@H](O[C@@H]2O[C@H](CO)[C@H](O)[C@H](O)[C@H]2O)[C@H](O)[C@H]1O>>[CH3:1][N:2]1[CH2:22][CH2:21][C:5](=[C:6]2[C:7]3[CH:20]=[CH:19][S:18][C:8]=3[C:9](=[O:10])[CH2:11][C:12]3[CH:13]=[CH:14][CH:15]=[CH:16][C:17]2=3)[CH2:4][CH2:3]1

Participants

3

Reactant 2

HCID 440995(+)-LactoseHCID 5282408Ketotifen fumarate

Product 1

HCID 3827Ketotifen

Procedure

2.75 kg of ketotifen hydrogen fumarate is mixed with 8.55 kg lactose for 5 minutes. The mass is sieved (vibration sieve; mesh width 500; hole size 250 microns). Separately 15 kg lactose and 2.5 kg corn starch are sieved and mixed (vibration sieve; hole size 1600 microns, wire diameter 630 microns). Glyceryl ditripalmitostearate is sieved (mesh width 1600, hole size 630 microns) and 41.2 kg thereof is mixed with two previously sieved masses, forming ketotifen fat granulate over ca. 30 minutes to ca. 50° C. The fat granulate is cooled to about 20° to 30° C. The mass is broken up using a sieve (hole size 1.5 mm). Total weight (two batches) 140 kg.

Workup

  1. filtrationThe mass is sieved (vibration sieve; mesh width 500; hole size 250 microns)
  2. filtrationSeparately 15 kg lactose and 2.5 kg corn starch are sieved
  3. additionmixed (vibration sieve; hole size 1600 microns, wire diameter 630 microns)
  4. filtrationGlyceryl ditripalmitostearate is sieved (mesh width 1600, hole size 630 microns) and 41.2 kg
  5. additionthereof is mixed with two previously sieved masses

Sources & evidence

ORD record
ord-223f86bbd35047d8b198eefcbdda544d
Source dataset
uspto-grants-1995_03
Patent number
US05399360

Reaction notes

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