関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Beta-Alanine | HCID 239 | — |
| 反応物 | Morpholine | HCID 8083 | — |
| 反応物 | Phosphorus trichloride | HCID 24387 | — |
| 反応物 | Phosphorous acid | HCID 107909 | — |
| 生成物 | Pamidronic Acid | HCID 4674 | — |
反応手順
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.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US06562974B2 |
|---|
| 出典データセット | uspto-grants-2003_05 |
|---|
| ORD ID | ord-1073b756d7524ebf91ed74ed69b1f293 |
|---|
| 出典メモ | uspto-grants-2003_05 |
|---|
