Dasabuvir Sodium
- CAS No.
- 1132940-11-4
- Chemical Name:
- Dasabuvir Sodium
- Synonyms
- Dasabuvir Sodium;Dasabuvir Sodium Hydrate
- CBNumber:
- CB93152187
- Molecular Formula:
- C26H28N3NaO5S
- Molecular Weight:
- 517.58
- MDL Number:
- MFCD30738732
- MOL File:
- 1132940-11-4.mol
- MSDS File:
- SDS
| FDA UNII | R2M8F5TK9T |
|---|
Dasabuvir Sodium Chemical Properties,Uses,Production
Description
Dasabuvir sodium (Exviera®), an oral non-nucleoside NS5B polymerase inhibitor discovered and developed by Abbvie, is a component of an all-oral hepatitis C treatment regimen Viekira Pak approved by the US FDA in December 2014 for the treatment of adult patients with chronic genotype 1 (GT1) hepatitis C virus (HCV) infection. The investigational regimen consists of the fixed-dose combination of paritaprevir (XXVII) (veruprevir, ABT- 450, vide infra) with ritonavir booster (150/100 mg) co-formulated with the NS5A inhibitor ombitasvir (XXV) (ABT-267, vide infra) 25 mg, dosed once daily, and nonnucleoside NS5B polymerase inhibitor dasabuvir (X) (ABT-333) 250 mg with or without ribavirin (weight-based), dosed twice daily. The drug was granted breakthrough therapy designation by the US FDA in May 2013. AbbVie’s application is supported by the data from six Phase III studies covering over 2300 patients in 25 countries representing one of the largest clinical programs in hepatitis C research and development. Across six studies, the 12-week therapeutic regimen achieved impressive cure rates, notching a 99% sustained virologic response mark in some populations.
Uses
Dasabuvir (ABT-333) sodium is a nonnucleoside hepatitis C virus (HCV) polymerase inhibitor. Dasabuvir sodium inhibits RNA-dependent RNA polymerase encoded by the HCV NS5B gene. Dasabuvir sodium inhibits genotype 1a (strain H77) and 1b (strain Con1) replicons, with EC50 values of 7.7 and 1.8 nM, respectively[1].
Definition
ChEBI: Dasabuvir sodium is an organic sodium salt having dasabuvir(1-) as the counterion; used (in the form of the hydrate) in combination with ombitasvir, paritaprevir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. It has a role as an antiviral drug and a nonnucleoside hepatitis C virus polymerase inhibitor. It contains a dasabuvir(1-).
Synthesis
Commercially available 2-tert-butyl phenol (65) was polyiodinated to furnish diiodophenol 66 in 93% yield. This was followed by methylation of the phenol to provide methyl phenyl ether 67 in 99% yield. Next, sequential couplings were employed to install the periphery about the central phenyl core. First, Goldberg coupling of 67 with pyrimidine-2,4-(1H,3H)-dione 68 in presence of CuI (10 mol %) and 69 provided compound 70 in 70% yield. Subsequently, the remaining iodide underwent Suzuki coupling with boronic acid 71 in the presence of Pd2(dba)3 and 72 to yield the naphthol 73 in high yield. Naphthol 73 was then converted to the corresponding polyfluorinated naphthol sulfonate 75, which was subsequently converted to dasabuvir through a palladium- mediated installation of methyl sulfonamide 76. Dasabuvir sodium (X) was then crystallized upon treatment with aq NaOH in i-PrOH and DMSO in 88% yield.
References
[1] Kati W, et al. In vitro activity and resistance profile of dasabuvir, a nonnucleoside hepatitis C virus polymerase inhibitor. Antimicrob Agents Chemother. 2015 Mar;59(3):1505-11. DOI:10.1128/AAC.04619-14
Dasabuvir Sodium Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Lynnchem | 86-(0)29-85992781 17792393971 | info@lynnchem.com | China | 4578 | 58 |
| Novachemistry | 44-20819178-90 02081917890 | info@novachemistry.com | United Kingdom | 4372 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32997 | 60 |
| Chongqing jooe co., ltd | +86-15223382610 | info@jooe.com | China | 15934 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
| Supplier | Advantage |
|---|---|
| Lynnchem | 58 |
| Novachemistry | 58 |
| TargetMol Chemicals Inc. | 58 |
| ATK CHEMICAL COMPANY LIMITED | 60 |
| Chongqing jooe co., ltd | 58 |
| TargetMol Chemicals Inc. | 58 |
View Lastest Price from Dasabuvir Sodium manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2026-07-27 | Dasabuvir sodium
1132940-11-4
|
$1520.00-2500.00 | 10g | TargetMol Chemicals Inc. |
-
- Dasabuvir sodium
1132940-11-4
- $1520.00-2500.00
- TargetMol Chemicals Inc.
