Tolvaptan sodium phosphate
- CAS No.
- 942619-79-6
- Chemical Name:
- Tolvaptan sodium phosphate
- Synonyms
- Tolvaptan sodiμm phosphate;Tolvaptan Sodium Phosphate;Tolvaptan Impurity(Disodium salt);Benzamide, N-[4-[[7-chloro-2,3,4,5-tetrahydro-5-(phosphonooxy)-1H-1-benzazepin-1-yl]carbonyl]-3-methylphenyl]-2-methyl-, sodium salt (1:2)
- CBNumber:
- CB29854079
- Molecular Formula:
- C26H27ClN2NaO6P
- Molecular Weight:
- 552.92
- MDL Number:
- MOL File:
- 942619-79-6.mol
- MSDS File:
- SDS
| FDA UNII | Y4P6WS9QVF |
|---|
Tolvaptan sodium phosphate price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0907509 | Tolvaptan phosphate ester sodium 99.85% | 942619-79-6 | 10mg | $38 | 2026-06-04 | Buy |
| ChemScene | CS-0907509 | Tolvaptan phosphate ester sodium 99.85% | 942619-79-6 | 25mg | $70 | 2026-06-04 | Buy |
| ChemScene | CS-0907509 | Tolvaptan phosphate ester sodium 99.85% | 942619-79-6 | 50mg | $108 | 2026-06-04 | Buy |
| ChemScene | CS-0907509 | Tolvaptan phosphate ester sodium 99.85% | 942619-79-6 | 100mg | $168 | 2026-06-04 | Buy |
| aablocks | AA02EOCI | TOLVAPTAN PHOSPHATE SODIUM >98% | 942619-79-6 | 10mg | $74 | 2026-06-03 | Buy |
Tolvaptan sodium phosphate Chemical Properties, Uses, Production
Description
Tolvaptan sodium phosphate (trade name Samtasu) is a selective small molecule vasopressin V2 receptor antagonist developed by Otsuka Pharmaceutical Co., Ltd. Tolvaptan sodium phosphate is a prodrug form of generic tolvaptan (7.13) with improved water solubility. The drug was approved by the Japanese PMDA in March 2022 for the treatment of patients with fluid retention who have difficulty taking tolvaptan orally.
Uses
Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation[1][2].
Mechanism of action
Tolvaptan sodium phosphate works by inhibiting water reabsorption in the renal collecting duct, thereby enhancing water diuresis (aquaresis) without depleting electrolytes. It is effective in treating patients with heart failure and has shown clinical benefits in weight loss and reduction of dyspnea and other symptoms of fluid overload. Tolvaptan sodium phosphate is also effective in treating early acute heart failure, where water diuresis can be rapidly induced by intravenous administration of tolvaptan in the early stages.
Synthesis
The route to the precursor 7.12 of tolvaptan (7) begins with the methyl esterification of commercially available 5-chloro-2-nitrobenzoic acid 7.1 to generate an equivalent of the methyl ester 7.2. Subsequent SnCl2-mediated reduction of the nitro group affords the aminobenzoic acid 7.3, which is protected as the N-toluenesulfonamide (7.4). Alkylation of 7.4 with ethyl 4-bromobutyrate affords the intermediate 7.5, which is a precursor for intramolecular ring formation. Treatment of 7.5 with base affords the benzazepine 7.6. Global deprotection under acidic conditions affords 7.7 in good yield, accompanied by ester hydrolysis and decarboxylation. Side chain construction begins with the coupling of aniline 7.7 and acyl chloride 7.8 to afford amide 7.9. Reduction of the nitro group to aniline 7.10, followed by amidation with acyl chloride 7.11, affords intermediate 7.12 with intact side chains. Reduction of the ketone followed by phosphorylation of the free alcohol and treatment with aqueous sodium hydroxide afforded Tolvaptan sodium phosphate7.
References
[1] Hiroyuki Fujiki, et al. In vitro and in vivo pharmacological profile of OPC-61815, a water-soluble phosphate ester pro-drug of tolvaptan. J Pharmacol Sci. 2022 Nov;150(3):163-172. DOI:10.1016/j.jphs.2022.08.004
[2] Wu Y, et al. Mechanisms of tolvaptan-induced toxicity in HepG2 cells. Biochem Pharmacol. 2015 Jun 15;95(4):324-36. DOI:10.1016/j.bcp.2015.03.015
Tolvaptan sodium phosphate Preparation Products And Raw materials
Raw materials
Preparation Products
Tolvaptan sodium phosphate Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| XianTao Li Zhao | 18571672902 | 1010771219@qq.com | China | 362 | 58 |
| hongqing Huafeng Pharmaceutical Technology Co., LTD | 23-67950001 13883380852 | cqhfyy@foxmail.com | China | 74 | 55 |
| Jinan Chenghui Shuangda biological Co., LTD | 053158897070 15550412551 | market@jnchsd.com | China | 224 | 62 |
| CHENGHUI PHARMACEUTICAL GROUP LTD | 053158897070 15550412551 | market@jnchsd.com | China | 241 | 58 |
| Shandong Chengchuang Blue Sea Pharmaceutical Technology Co., Ltd. | 0531-58897130 15508676053 | drug_impurity@sdcclh.com | China | 2526 | 58 |
| TOSUN PHARM | 020-66392521-118 18922260391 | 3004261881@qq.com | China | 7994 | 58 |
| Dideu Industries Group Limited | +8617392712697 | 1022@dideu.com | China | 29091 | 58 |
| Jinan chenghui-shuangda chemical co.,ltd. | 13256107535 | mahaiyan1123@126.com | China | 118 | 58 |
| NANJING WEDO PHARMATECH CO.,LTD. | 15189836218 | wedo-chem@huawe.com | China | 240 | 58 |
| PureChemland Co.,Ltd. | 13540909846 13882008651 | 3848291069@qq.com | China | 3000 | 58 |
View Latest Price from Tolvaptan sodium phosphate manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2025-12-25 | Tolvaptan Sodium Phosphate
942619-79-6
|
1g | 0.99 | 50kg | Wuhan Biocar Pharmacy CO.,Ltd. |
-
- Tolvaptan Sodium Phosphate
942619-79-6
- 0.99
- Wuhan Biocar Pharmacy CO.,Ltd.
