Daclatasvir Dihydrochloride

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H317：Kann allergische Hautreaktionen verursachen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

  H373：Kann die Organe schädigen bei längerer oder wiederholter Exposition.

• Sicherheit

  P260：Dampf/Aerosol/Nebel nicht einatmen.

  P261：Einatmen von Staub vermeiden.

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P272：Kontaminierte Arbeitskleidung nicht außerhalb des Arbeitsplatzes tragen.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P302+P352：BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

  P314：Bei Unwohlsein ärztlichen Rat einholen / ärztliche Hilfe hinzuziehen.

  P321：Besondere Behandlung

  P333+P313：Bei Hautreizung oder -ausschlag: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P363：Kontaminierte Kleidung vor erneutem Tragen waschen.

  P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Daclatasvir Dihydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Daclatasvir dihydrochloride is a hepatitis C virus nonstructural 5A (NS5A) replication complex inhibitor which was first approved in Japan for the treatment of genotype 1 HCV patients who fail to respond to interferon plus ribavirin. The drug has also been approved for patients with untreated, chronic HCV who are eligible for interferon. Additionally, in Europe, daclatasvir was approved for use in combination with other products across genotype 1–4 HCV. Daclatasvir was discovered and developed by Bristol–Myers Squibb and a fascinating account describing the initiation of the program from a phenotypic screen and the medicinal chemistry strategy leading to the discovery of the compound has been recently reported.

• Chemische Eigenschaften

  Daclatasvir dihydrochloride is white to yellow powder. It is freely soluble in water (>700 mg/mL). The solubility is strongly pH-dependent and the solubility is high at low pH values.

• Verwenden

  Daclatasvir Dihydrochloride is the dihydrochloride salt form of daclatasvir, an orally available inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, with potential activity against HCV. Daclatasvir is used with another antiviral medication (sofosbuvir) to treat chronic (long-lasting) hepatitis C, a viral infection of the liver. Daclatasvir should never be used without sofosbuvir. Daclatasvir and sofosbuvir may also be used with another antiviral medication (ribavirin).

• Definition

  ChEBI: Daclatasvir hydrochloride is a hydrochloride obtained by combining daclatasvir with two molar equivalents of hydrochloric acid. It is a potent inhibitor of nonstructural protein 5A and is used for treatment of hepatitis C. It has a role as an antiviral drug and a nonstructural protein 5A inhibitor. It contains a daclatasvir(2+).

• Synthese

  Bromination of commercial 4,40-diacetylbiphenyl (58) gave 4,40-bis(bromoacetyl)biphenyl 59 in 82% yield. Alkylation of NBoc- L-proline (60) with 59 gave diester 61 which was treated with ammonium acetate to effect cyclization of the bis-ketoester to provide bis-imidazole 62 in 63% yield for the two steps. Acidic removal of the Boc protecting groups followed by recrystallization provided bis-pyrrolidine 63 in high yield. Acylation of 63 with N-(methoxycarbonyl)- L-valine (64) using N-(3-dimethylaminopropyl)-N0-ethylcarbodiimide (EDC) and 1-hydroxybenxotriazole hydrate (HOBT) provided declatasvir. The dihydrochloride salt was prepared and treated with Cuno Zet Carbon ® followed by crystallization from acetone to give daclatasvir dihydrochloride (IX) in 74% yield.

• Mode of action

  Daclatasvir is an inhibitor of nonstructural protein 5A (NS5A), a multifunctional protein that is an essential component of the HCV replication complex. Daclatasvir binds to the N-terminus of NS5A and inhibits both viral RNA replication and virion assembly.

Daclatasvir Dihydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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