S-033188
Baloxavir marboxil
CAS: 1985606-14-1
Molecular Formula: C27H23F2N3O7S
S-033188 - Names and Identifiers
| Name | Baloxavir marboxil |
| Synonyms | Xofluza XOFLUZA CS-2794 S-033188 aloxavir marboxil Baloxavir marboxil baloxavir marboxil S-033188 |
| CAS | 1985606-14-1 |
S-033188 - Physico-chemical Properties
| Molecular Formula | C27H23F2N3O7S |
| Molar Mass | 571.55 |
| Density | 1.57±0.1 g/cm3(Predicted) |
| Boling Point | 712.8±70.0 °C(Predicted) |
| pKa | -1.46±0.40(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Use | In February 2018, a new anti-influenza drug, baroxavir dipivoxil (Baloxavirmarboxil, trade name: Xofluza), developed by Japan's Shiono Yoshiki Pharmaceutical (Shionogi) and jointly studied with Roche, Switzerland, was approved for accelerated approval and marketing in Japan. Baroxavir dipivoxil is an innovative Cap-dependent endonuclease inhibitor, and it is also one of the few new drugs in the world that can inhibit the proliferation of influenza viruses. In June 2018, the U.S. Food and Drug Administration (FDA) accepted a new drug listing application for baroxavir dipivoxil and granted it priority review qualifications. |
S-033188 - Indications
Open Data Unverified Data
baroxavir dipivoxil is suitable for patients ≥ 12 years old who suffer from acute uncomplicated influenza and whose symptoms do not exceed 48 hours. Attention should be paid to the limitations of medication: influenza virus changes over time, and there are factors such as virus type and subtype. Once the drug resistance of the virus and the pathogenicity of the virus change, the clinical efficacy of antiviral drugs may be weakened. When deciding whether to take basalovir dipivoxil, the available information on the sensitivity of the local epidemic virus strain to the drug should be considered.
Last Update：2022-06-27 18:40:51
S-033188 - Preparation
Open Data Unverified Data
Japanese patent JP6212678 reported the synthesis method of baroxavir dipivoxil. 3, 4-difluorobenzoic acid was used as raw material to react with DMF under the action of LDA to obtain 2-formyl -3, 4-difluorobenzoic acid. Then it forms thioacetal with thiophenol, then it is reduced and separated with borane to obtain 2-phenylthiomethyl -3, 4-difluorob, 8-difluorodibenzo [B, e] thiazepine -11(6H)-one, and finally the key thiazepine fragment 7, 8-difluoro-6, 11-dihydrodibenzo [B, e] thiazepine -11-alcohol is obtained under the reduction of sodium borohydride. Using 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid to react with tert-butyl formate after esterification to obtain 3-(benzyloxy)-1-((tert-butoxycarbonyl) amino) -4-oxo-1, 4-dihydropyridine-2-methyl formate hydrate, and then with 2-(2, 2-dimethoxyethoxy) ethylamine undergoes urethane exchange reaction, and then cyclizes under the action of methanesulfonic acid to obtain 7-(benzyloxy)-3,4,12, 12a-tetrahydro-1H-[1,4] oxazino [3,4-c] pyridino [2,1-f][1,2,4] triazine -6, 8-dione hemihydrate, then it is condensed with (R)-tetrahydrofuran -2-formic acid, then crystallized and resolved, and then the chiral auxiliary group is removed to obtain the key chiral parent ring molecule (R)-7-(benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4] oxazino [3,4-c] pyrido [2,1-f][1,4] Triazine-6, 8-dione. Then the key parent ring molecule is used to exchange with n-hexanol under the action of Grignard reagent, and then with the key thiazepine fragment 7, 8-difluoro-6, 11-dihydrodibenzo [B, e] thiazepine -11-alcohol docking, and finally debutylation and condensation with methyl chloroformate to obtain the final product baloxavir pivoxil.
Last Update：2022-06-27 18:40:52
S-033188 - Anti-influenza virus drugs
Open Data Unverified Data
Baroxavir dipivoxil is a prodrug that enters the body and is hydrolyzed into the active substance Baroxavir to exert anti-influenza virus activity.
Baloxavir is an anti-influenza drug with a completely new mechanism of action, which can inhibit the cap-dependent endonuclease in influenza virus, thereby blocking the transcription of the virus's own mRNA. Baloxavir has a half-life of about 80 hours and only needs to be taken once.
Last Update：2022-06-27 18:40:52
S-033188 - Mechanism of action
Open Data Unverified Data
Baroxavir dipivoxil is a small molecule prodrug. Its mechanism of action is different from that of existing antiviral therapies. It can selectively inhibit cap-dependent endonuclease and prevent polymerase function and influenza virus mRNA replication. The mechanism of action of anti-influenza drugs is through targeting neuraminidase. Compared with these drugs, baroxavir targets earlier stages of the viral replication cycle
Last Update：2022-06-27 18:40:52
S-033188 - Indications
Open Data Unverified Data
Baroxavir (baloxavir marboxil) is a selective inhibitor of cap-dependent endonuclease of influenza virus. The drug has shown therapeutic activity in preclinical models of influenza A and B virus infection, including strains resistant to current antiviral agents.
Baroxavir was approved by the FDA in 2018. It is a new anti-influenza drug with a new mechanism of action. It can selectively inhibit cap-dependent endonuclease and prevent polymerase function and influenza virus mRNA replication.
Balosavir is developed by Shionoshi Pharmaceuticals and has signed an agreement with Roche, including Roche's subsidiary Genentech, to jointly develop and commercialize Balosavir globally. Shionoshi/Roche is currently conducting Phase 3 clinical trials of Balosavir pivoxil in China.
Last Update：2022-06-27 18:40:53
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Spot supply
Product Name: Baloxavir Impurity 9 Visit Supplier Webpage Request for quotationCAS: 1985606-14-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Baloxavir marboxil Visit Supplier Webpage Request for quotation
CAS: 1985606-14-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1985606-14-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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