2-Hydroxy-1,2,3-propanetricarboxylic acid hydrate (1:1) → L-Aspartic Acid

HRID 1689619Notes

Reaction equation

HRID 1689619 reaction equation
P([O-])([O-])(O)=O.[Na+].[Na+].O.[C:9]([OH:21])(=[O:20])[CH2:10][C:11](CC(O)=O)([C:13]([OH:15])=[O:14])O.CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@H](O)[C@@](OC)(C)C2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@@](O)(C)C[C@@H](C)C[N:28](C)[C@H](C)[C@@H](O)[C@@]1(O)C>O>[NH2:28][C@H:11]([C:13]([OH:15])=[O:14])[CH2:10][C:9]([OH:21])=[O:20]

Participants

5

Reactant 3

HCID 222302-Hydroxy-1,2,3-propanetricarboxylic acid hydrate (1:1)HCID 24203Sodium Phosphate, DibasicHCID 447043Azithromycin

Product 1

HCID 5960L-Aspartic Acid

Reagents, catalysts & solvents 1

HCID 962WaterSolvent

Procedure

To water (80 mL) agitated at 15° C. to 25° C., disodium hydrogenphosphate 12 hydrate (3.3 g) and citric acid monohydrate (0.44 g) were added. After these buffers were completely dissolved, azithromycin (1.0 g) was added and dissolved with agitation. After confirming that the solution became clear, sterile purified water was added to prepare 100 mL of the azithromycin-containing aqueous pharmaceutical composition (Comparative Example 2).

Workup

  1. dissolutionAfter these buffers were completely dissolved
  2. dissolutiondissolved with agitation
  3. customsterile purified water
  4. additionwas added
  5. customto prepare 100 mL of the azithromycin-
  6. additioncontaining aqueous pharmaceutical composition (Comparative Example 2)

Sources & evidence

ORD record
ord-5ed860710baa44a2bb178d16d9cc4b06
Source dataset
uspto-grants-2012_04
Patent number
US08153601B2

Reaction notes

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