763105-70-0

Basic information

• Product Name: N'-[(2Z)-Piperazin-2-ylidene]trifluoroacetohydrazide
• Synonyms: N-[(2Z)-Piperazin-2-ylidene]-2,2,2-trifluoroacetohydrazide;N'-[(2Z)-Piperazin-2-ylidene]trifluoroacetohydrazide;Trifluoroacetic Acid (2Z)-Piperazinylidenehydrazide;(Z)-2,2,2-trifluoro-N'-(piperazin-2-ylidene)acetohydrazide
• CAS NO: 763105-70-0
• Molecular Formula: C₆H₉F₃N₄O
• Molecular Weight: 210.16
• Product Categories: Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 763105-70-0.mol
• Article Data: 21

Chemical Properties

• Appearance: White Solid
• Storage Temp.: Hygroscopic, Refrigerator, under inert atmosphere
• Solubility: DMSO (Slightly), Methanol (Slightly, Heated)
• Stability: Hygroscopic
• CAS DataBase Reference: N'-[(2Z)-Piperazin-2-ylidene]trifluoroacetohydrazide(CAS DataBase Reference)
• NIST Chemistry Reference: N'-[(2Z)-Piperazin-2-ylidene]trifluoroacetohydrazide(763105-70-0)
• EPA Substance Registry System: N'-[(2Z)-Piperazin-2-ylidene]trifluoroacetohydrazide(763105-70-0)

Safety Data

• Hazardous Substances Data: 763105-70-0(Hazardous Substances Data)

Usage

Chemical Properties

White Solid

Uses

Sitagliptin intermediate

Upstream product

• 383-63-1 ethyl trifluoroacetate, 
• 723286-98-4 2-trifluoromethyl-1,3,4-oxadiazol-5-ylmethyl chloride 
• 107-15-3 ethylenediamine 

Downstream Products

• 486460-32-6 sitagliptin 
• 767340-03-4 (Z)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)but-2-en-1-one 
• 654671-78-0 sitagliptin phosphate 
• 762240-92-6 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride 
• 654671-77-9 sitagliptin phosphate monohydrate 

Relevant articles and documents

Preparation method of sitagliptin intermediate

The invention relates to a preparation method of a sitagliptin intermediate, and belongs to the technical field of drug intermediate synthesis. In order to solve the problems of low product yield andpoor environmental protection property in the prior art, the invention provides a preparation method of a sitagliptin intermediate, and the method comprises the following steps: reacting 2-piperazinone with hydrazine hydrate in an alcohol solvent to generate piperazine hydrazone; in an acetonitrile or ether solvent, reacting the piperazine hydrazone with ethyl trifluoroacetate to obtain a corresponding intermediate N -[(2Z-) piperazine -2-subunit] trifluoroacethydrazide; and performing cyclization and salification reaction on the N -[(2Z-) piperazine -2-subunit] trifluoroacethydrazide in an alcohol solvent under the action of hydrochloric acid to obtain the corresponding sitagliptin intermediate 3-trifluoromethyl 5, 6, 7, 8-tetrahydro-1, 2, 4-triazole [4, 3-a] pyrazine hydrochloride. The reaction has the effects of high selectivity and high product yield.

PROCESS FOR THE PREPARATION OF SITAGLIPTIN AND ITS INTERMEDIATES

The present invention relates to novel and improved processes for the preparation of Sitagliptin compound of formula (1) and its intermediates.

DODECYLSULFATE SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR

The dodecylsulfate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[l,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl) butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the treatment of Type 2 diabetes. The invention also relates to a crystalline anhydrate of the dodecylsulfate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of Type 2 diabetes, hyperglycemia, insulin resistance, and obesity.