R-Ginsenoside Rg3 → Ginsenoside Rg3

HRID 522486Notes

Reaction equation

HRID 522486 reaction equation
[CH3:1][C:2]([CH3:55])=[CH:3][CH2:4][CH2:5][C@@:6]([OH:54])([C@@H:8]1[C@H:12]2[C@H:13]([OH:52])[CH2:14][C@@H:15]3[C@@:20]4([CH3:50])[CH2:21][CH2:22][C@H:23]([O:27][C@@H:28]5[O:33][C@H:32]([CH2:34][OH:35])[C@@H:31]([OH:36])[C@H:30]([OH:37])[C@H:29]5[O:38][C@@H:39]5[O:44][C@H:43]([CH2:45][OH:46])[C@@H:42]([OH:47])[C@H:41]([OH:48])[C@H:40]5[OH:49])[C:24]([CH3:26])([CH3:25])[C@@H:19]4[CH2:18][CH2:17][C@@:16]3([CH3:51])[C@:11]2([CH3:53])[CH2:10][CH2:9]1)[CH3:7]>O>[CH3:1][C:2]([CH3:55])=[CH:3][CH2:4][CH2:5][C@:6]([OH:54])([C@@H:8]1[C@H:12]2[C@H:13]([OH:52])[CH2:14][C@@H:15]3[C@@:20]4([CH3:50])[CH2:21][CH2:22][C@H:23]([O:27][C@@H:28]5[O:33][C@H:32]([CH2:34][OH:35])[C@@H:31]([OH:36])[C@H:30]([OH:37])[C@H:29]5[O:38][C@@H:39]5[O:44][C@H:43]([CH2:45][OH:46])[C@@H:42]([OH:47])[C@H:41]([OH:48])[C@H:40]5[OH:49])[C:24]([CH3:25])([CH3:26])[C@@H:19]4[CH2:18][CH2:17][C@@:16]3([CH3:51])[C@:11]2([CH3:53])[CH2:10][CH2:9]1)[CH3:7]

Participants

3

Reactant 1

HCID 46887680R-Ginsenoside Rg3

Product 1

HCID 9918693Ginsenoside Rg3

Reagents, catalysts & solvents 1

HCID 962WaterSolvent2×

Procedure

Take 100 ml of 20(R)-ginsenoside Rg3 composition solution obtained from Operation Example 1, add water for injection to 1000 ml, and add 0.1 grams of injection grade active carbon and mix to uniformity. Leave it at 80° C. for 30 minutes, remove the pyrogen with 0.45 μm micropore membrane filtering, sterilize with a 0.22 μm micropore filter membrane under sterile conditions, dispense into a 10 ml sterile antibiotics tube vial under sterile conditions, and the quantity of each tube vial is 4.5˜4.9 ml:5 mg. After the dispensed, the antibiotics tube vials are half-corked, they are transferred onto the plate of lyophilizer (LYO-5, manufactured in Shanghai). Close the door of the lyophilizer, turn on the lyophilizer and first freeze to below −40° C. and keep for 4 hours, and then start vacuum drying as following program for sublimation: −45˜−30° C. for 4 hours, −30˜−20° C. for 4 hours, −20˜−15° C. for 2 hours. Finally, dry for 4 hours at 15˜30° C., and the lyophilization process is complete. After lyophilization, the corks are fully plugged and aluminum covers are pressed on with a sealing machine. Sample some sample for testing. Pack the qualified tube vials. 1000 tube vials of lyophilized powder for injection (3.1 mg Rg3/vial) are obtained. The above-mentioned procedures can be carried out for Example 2-40 to produce water-soluble powder of ginsenoside Rg3.

Workup

  1. additionadd 0.1 grams of injection grade active carbon
  2. additionmix to uniformity
  3. customLeave it at 80° C. for 30 minutes
  4. customremove the pyrogen with 0.45 μm micropore membrane
  5. filtrationfiltering
  6. filtrationsterilize with a 0.22 μm micropore filter membrane under sterile conditions, dispense into a 10 ml sterile antibiotics tube vial under sterile conditions
  7. customthe quantity of each tube vial is
  8. customClose the door of the lyophilizer, turn on the lyophilizer and first freeze to below −40° C.
  9. customdrying
  10. wait−45˜−30° C. for 4 hours
  11. wait−30˜−20° C. for 4 hours
  12. wait−20˜−15° C. for 2 hours
  13. customFinally, dry for 4 hours at 15˜30° C.
  14. custom1000 tube vials of lyophilized powder for injection (3.1 mg Rg3/vial) are obtained

Sources & evidence

ORD record
ord-dc81a58377fb450c814925f3307cff37
Source dataset
uspto-grants-2016_05
Patent number
US09333215B2

Reaction notes

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