Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Beta-Alanine | HCID 239 | — |
| Reactant | Morpholine | HCID 8083 | — |
| Reactant | Phosphorus trichloride | HCID 24387 | — |
| Reactant | Phosphorous acid | HCID 107909 | — |
| Product | Pamidronic Acid | HCID 4674 | — |
Reaction Steps
The mixture of 5 eq. phosphorous acid and β-alanine is heated to form a melt. Morpholine (1 eq.) is slowly added. The reaction is cooled to about 70° C. and 2 eq. of PCl3 are added. The mixture is heated for about 3.5 hours. Then the reaction is hydrolyzed in aqueous acid at about 75° C. for about 0.5 hours. Crystallization from aqueous acid/IPA, affords pamidronate.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US06562974B2 |
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| Source dataset | uspto-grants-2003_05 |
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| ORD ID | ord-1073b756d7524ebf91ed74ed69b1f293 |
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| Source note | uspto-grants-2003_05 |
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