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ChemicalBook >  Product Catalog >  Organic Chemistry >  Organic fluorine compound >  Fluoropyridine series >  3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride

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

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

Product Name:
3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride
Synonyms:
  • 3-(TRIFLUOROMETHYL)-5,6,7,8- TETRAHYDRO[1,2,4]TRIAZOLO[4,3-
  • 3-trifluoro Methyl-[1,2,4]triazole[4,3-a]piperazine hydrochloride
  • Sitagliptin Triazole Hydrochloride
  • Sitagliptin Impurity 64
  • 5,6,7,8-Tetrahydro-3-(trifluoromethyl)[1,2,4]triazolo[4,3-a]pyrazine hydrochloride 98%
  • Sitagliptin interMediate A
  • 1,2,4-Triazolo[4,3-a]pyrazine,5,6,7,8-tetrahydro-3-(trifluoroMethyl)-,hydrochloride(1:1)
  • 3 - (three fluorinated Methyl) - 5,6,7,8 - four hydrogen - triazole 4-trichlorobenzene [1] and [4, 3 - alpha] pyrazine hydrochloride
CAS:
762240-92-6
MF:
C6H7F3N4.ClH
MW:
228.6
EINECS:
616-309-4
Product Categories:
  • Pyrazine
  • Aromatics
  • Aromatics Compounds
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • 1
Mol File:
762240-92-6.mol
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3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride Chemical Properties

Melting point:
236-246°C
storage temp. 
Keep in dark place,Sealed in dry,Room Temperature
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
color 
White to Off-White
InChI
InChI=1S/C6H7F3N4.ClH/c7-6(8,9)5-12-11-4-3-10-1-2-13(4)5;/h10H,1-3H2;1H
InChIKey
AQCSCRYRCRORET-UHFFFAOYSA-N
SMILES
C12=NN=C(C(F)(F)F)N1CCNC2.[H]Cl
CAS DataBase Reference
762240-92-6(CAS DataBase Reference)
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Safety Information

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN2811
HS Code 
2933599577
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3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride Usage And Synthesis

Description

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.

Chemical Properties

White Solid or White to Light yellow powder to crystal

Uses

Sitagliptin intermediate.

Synthesis

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 hydrochlorideSupplier

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