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3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2.4]triazolo[4,3-a]pyrazine hydrochloride

  • CasNo:762240-92-6

Product Description

Export Top Purity 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2.4]triazolo[4,3-a]pyrazine hydrochloride 762240-92-6 In Stock

  • Molecular Formula: C6H7F3N4.HCl
  • Molecular Weight: 228.605
  • Appearance/Colour: white solid 
  • Melting Point: 236-246oC 
  • Boiling Point: 266.2 °C at 760 mmHg 
  • Flash Point: 114.8 °C 
  • PSA: 42.74000 
  • LogP: 1.53090 

762240-92-6 Relevant articles

Preparation method of sitagliptin intermediate

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Paragraph 0024; 0030; 0034-0035; 0039-0040; 0044-0045; 0049, (2021/02/13)

The invention relates to a preparation m...

Green synthesis method of sitagliptin intermediate

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Paragraph 0032; 0044-0047; 0051-0052; 0056-0059, (2021/10/27)

The invention relates to a green synthes...

Preparation method of sitagliptin intermediate

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Paragraph 0074-0076, (2021/06/22)

The invention discloses a preparation me...

Preparation method of sitagliptin intermediate

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Paragraph 0036, (2020/07/15)

The invention provides a method for prep...

762240-92-6 Process route

2,2,2-trifluoro-N’-[(2Z)-piperazin-2-ylidene]acetohydrazide
763105-70-0

2,2,2-trifluoro-N’-[(2Z)-piperazin-2-ylidene]acetohydrazide

3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride
762240-92-6

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

Conditions
Conditions Yield
With hydrogenchloride; In methanol; at 55 ℃; for 0.5h;
92%
With hydrogenchloride; In ethanol; water; at 50 - 54 ℃; for 3.5h; Temperature;
92.6%
With hydrogenchloride; In isopropyl alcohol; at 60 - 65 ℃; for 2h; Temperature; Inert atmosphere; Large scale;
91%
With hydrogenchloride; In methanol; at 55 ℃;
90.7%
2,2,2-trifluoro-N’-[(2Z)-piperazin-2-ylidene]acetohydrazide; In ethyl acetate; at 60 ℃; for 0.333333h; Inert atmosphere;
With hydrogenchloride; In ethyl acetate; for 3h; Inert atmosphere;
90.1%
With hydrogenchloride; In methanol; tert-butyl methyl ether; at 20 ℃; for 1.66667 - 2.5h;
With hydrogenchloride; In methanol; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; water; at 20 - 55 ℃; for 0.916667 - 1.75h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
2,2,2-trifluoro-N’-[(2Z)-piperazin-2-ylidene]acetohydrazide; With hydrogenchloride; In methanol; at 55 ℃; for 0.75h;
2,2,2-trifluoro-N’-[(2Z)-piperazin-2-ylidene]acetohydrazide; With hydrogenchloride; In methanol; tert-butyl methyl ether; at 20 ℃; for 1h;
2,2,2-trifluoro-N’-[(2Z)-piperazin-2-ylidene]acetohydrazide; With hydrogenchloride; In methanol; at 55 ℃; for 0.75h;
In tert-butyl methyl ether; at 20 ℃; for 1h;
With hydrogenchloride; In methanol; water; at 20 - 55 ℃; for 0.916667 - 1.75h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; water; at 20 - 55 ℃; for 0.916667 - 1.75h;
With hydrogenchloride; In methanol; at 50 - 55 ℃; for 3h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; water; at 55 ℃; for 0.75h;
With hydrogenchloride; In methanol; at 55 ℃; for 1h;
1.36 g
3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyrazine
486460-20-2

3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyrazine

3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride
762240-92-6

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

Conditions
Conditions Yield
3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyrazine; With palladium on activated carbon; hydrogen; In methanol; at 40 - 45 ℃; for 24h; under 2625.26 - 3375.34 Torr;
With hydrogenchloride; In isopropyl alcohol; at 0 - 5 ℃;
82.9%
Multi-step reaction with 2 steps
1: palladium 10% on activated carbon; hydrogen / ethanol / 45 °C / 3345.86 Torr / Large scale
2: hydrogenchloride / Isopropyl acetate / 1 h / 20 °C / Large scale
With hydrogenchloride; palladium 10% on activated carbon; hydrogen; In ethanol; Isopropyl acetate;
With palladium 10% on activated carbon; hydrogen; In Isopropyl acetate; at 40 - 45 ℃; under 2585.81 Torr;
8 g

762240-92-6 Upstream products

  • 763105-70-0
    763105-70-0

    2,2,2-trifluoro-N’-[(2Z)-piperazin-2-ylidene]acetohydrazide

  • 823817-55-6
    823817-55-6

    (S)-Sitagliptin

  • 486460-20-2
    486460-20-2

    3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyrazine

  • 486460-21-3
    486460-21-3

    3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine

762240-92-6 Downstream products

  • 764667-65-4
    764667-65-4

    1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butane-1,3-dione

  • 874360-10-8
    874360-10-8

    tert-butyl [(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-2-(2,4,5-trifluorophenyl)cyclohexyl]carbamate

  • 486460-23-5
    486460-23-5

    (R)-tert-butyl 4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-ylcarbamate

  • 959839-54-4
    959839-54-4

    6-(4-Fluoro-3-{[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]carbonyl}benzyl)-4,5-dimethylpyridazin-3(2H)-one

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