3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P304+P340：BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen.

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

  P405：Unter Verschluss aufbewahren.

3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride is a pharmaceutical intermediate compound used in the preparation of Sitagliptin phosphate. Sitagliptin is an oral hypoglycaemic agent, a dipeptidyl peptidase-4 inhibitor, which is used in the treatment of type 2 diabetes.

• Chemische Eigenschaften

  White Solid or White to Light yellow powder to crystal

• Verwenden

  Sitagliptin intermediate.

• Synthese

  A suspension of N'-[(2Z)-Piperazin-2-ylidene]trifluoroacetohydrazide (27.3 g, 0.13 mol) in 110 mL of methanol was WARMED TO 55 ℃. 37% Hydrochloric acid (11.2 mL, 0.14 mol) was added over 15 min at this temperature. During the addition, all solids dissolved, resulting in a clear solution. The reaction was aged for 30 min. The solution was cooled to 20 ℃ and aged at this temperature until a seed bed formed (10 min to 1 h). 300 ML of MTBE was charged at 20 ℃ over 1 h. The resulting slurry was cooled to 2 ℃, aged for 30 min and filtered. Solids were washed with 50 mL of ethanol: MTBE (1: 3) and dried under vacuum at 45 ℃. Yield of 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride was 26.7 g (99.5 area wt% pure by HPLC).

3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride Upstream-Materialien And Downstream Produkte

3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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