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Pamidronic Acid → Alendronic Acid

HRID 74141
Notes
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Reaction equation

HRID 74141 reaction equation
[CH2:1]([C:4]([P:10]([OH:13])([OH:12])=[O:11])([P:6]([OH:9])([OH:8])=[O:7])[OH:5])[CH2:2]N.C[CH2:15][N:16](CC)CC>O>[CH2:2]([CH2:15][NH2:16])[CH2:1][C:4]([P:10]([OH:13])([OH:12])=[O:11])([P:6]([OH:9])([OH:8])=[O:7])[OH:5]
ParticipantsProcedureWorkupSources & evidenceReaction notes

Participants

4

Reactant 2

HCID 4674Pamidronic AcidHCID 8471Triethylamine

Product 1

HCID 2088Alendronic Acid

Reagents, catalysts & solvents 1

HCID 962WaterSolvent

Procedure

The NHS ester (0.35 g, 0.62 mmol) was dissolved in H2O (30 mL), and pamidronate (0.52 g, 2.23 mmol) and Et3N (1.7 mL, 12.4 mmol) were added. The reaction solution was stirred for 24 h at room temperature. Subsequently, the H2O was removed in the vacuum. The product obtained was purified by means of HPLC.

Workup

  1. customSubsequently, the H2O was removed in the vacuum
  2. customThe product obtained
  3. customwas purified by means of HPLC

Sources & evidence

ORD record
ord-63709912d71b4b3b8f382421cafd90e3
Source dataset
uspto-grants-2014_09
DOI
10.6084/m9.figshare.5104873.v1
Patent number
US08829233B2

Reaction notes

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On this pageParticipantsProcedureWorkupSources & evidenceReaction notes