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Intermediate of Ticagrelor 4 CAS 376608-71-8

Intermediate of Ticagrelor 4 CAS 376608-71-8

    Terms of Trade: FOB
    Min. Order: 1 Kilogram
    Delivery Time: 1 Days
    Packaging: AS REQUIRED
    Productivity: KGS
    Transportation: Air
    Place of Origin: CHINA
    Supply Ability: TRUE MANUFACTURER
    Certificate: ISO

Basic Info

Model No.: 376608-71-8

Product Description

(1R,2R)-2-(3,4-difluorophenyl)cyclopropanaMine(S)-(carboxylato(phenyl)Methyl)holMiuM cas number 376608-71-8 is an intermediate of Ticagrelor. His synthesis process is:
(1) Dissolve DMA in chloroform, cool down to 0-5 ° C, add trifluoromethanesulfonic anhydride, control the temperature does not exceed 5 ° C, a large amount of white solids precipitated, drip, constant temperature at 0-5 ° C The reaction was carried out for 25 to 35 minutes to obtain a first solution. The 3,4-difluorostyrene and 2,4,6-trimethylpyridine were dissolved in chloroform, and the solution was added dropwise to the first solution, refluxed for 15 to 20 hours, a portion of water was added, and reflux was continued for 15 to 20 hours. Then, it was cooled to room temperature, and the layers were separated to give an organic layer, and then the aqueous layer was extracted with chloroform, and the organic layer extracted with chloroform was combined with the organic layer obtained by layering. Then, it was dried over anhydrous sodium sulfate and subjected to column chromatography to give a pale yellow liquid.
(2) The pale yellow liquid obtained in the first step is dissolved in tetrahydrofuran, and LiHMDS (1M inTHF) is added dropwise at a temperature of -80 to -60℃. After the completion of the dropwise addition, the temperature is kept at -80 to -60℃ for heat preservation. 15 ~ 25min. Then, NBS was added to the solution after the reaction, and the temperature was raised to -5 to 5℃ for 15 to 25 minutes. Further, a sodium hydroxide solution was added, and the reaction was stirred at room temperature for 12 to 24 hours. The product was layered and the aqueous layer was adjusted to pH 3-4 with dilute hydrochloric acid. The aqueous layer was extracted with EtOAc. Column chromatography was then carried out to give an off-white solid.
(3) The white solid obtained in step 2 is dissolved in toluene, a drop of pyridine is added, then thionyl chloride is added, and the temperature is raised to 68-72℃ for 2.5-3.5 hours, and then thionyl chloride is added to continue the heat preservation. The reaction is carried out for 0.8 to 1.2 hours. The reaction solution was evaporated to dryness, and the residue was dissolved in toluene, and then cooled to -5 to 2℃, and then sodium azide, tetrabutylammonium bromide and sodium carbonate were added to carry out the reaction for 1.5 to 2.5 hours. The azide product was diluted with water, layered, and the organic layer was washed with saturated sodium chloride. Next, the toluene was heated to 100 ° C, added dropwise to the organic phase which was layered and washed after azide, and subjected to a rearrangement reaction to form an isocyanate. Then, the resulting isocyanate solution is added dropwise to the hydrochloric acid solution, and the temperature is controlled at 75 to 85℃ for 60 to 70 minutes. After adding water to cool to 25 ° C, stratification was carried out. Further, the aqueous layer in which the salt was dissolved after the hydrolysis under acidic conditions was adjusted to pH 10 to 12 with a sodium hydroxide solution, and extracted with ethyl acetate. After separation, the ethyl acetate layer was washed with water. Then, R-mandelic acid is dissolved in ethyl acetate, and then mixed with the above-mentioned washed ethyl acetate layer, and the temperature is controlled at 16 to 19℃, the reaction is stirred for 2.5 to 3.5 hours, and suction filtration is carried out, and the filter cake is treated with acetic acid. The ester was washed and dried under low temperature to give ticagrelor intermediate (1R,2R)-2-(3,4-difluorophenyl)cyclopropanaMine(S)-(carboxylato(phenyl)Methyl)holMiuM cas number 376608-71-8

Thera. Category: antagonist of the platelet purinergic P2Y12 receptor

Cas No.: 376608-71-8

Synonyms: Ticagrelor InterMediate 4;(1R,2S)-2-(3,4-Difluorophenyl)cyclopropanaMine (2R)-Hydroxy(phenyl)ethanoate;(αR)-α-Hydroxybenzeneacetic Acid coMpd. with (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanaMine; (1R,2R)-2-(3,4-difluorophenyl)cyclopropanamine(S)-(carboxylato(phenyl)methyl)holmium;trans-(1R,2S)-2-(2,3-difluorophenyl)cyclopropylaMine Mandelat;(1R,2S)-2-(3,4-Difluorophenyl)cyclopropanaminium (2R)-hydroxy(phenyl)ethanoate;(alphaR)-alpha-Hydroxybenzeneacetic acid compd. with (1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine;(αR)-(1R,2S)-α-hydroxy-Benzeneacetic acid-coMpd.with 2-(3,4-difluorophenyl)cyclopropanaMine(1:1);

Molecular Formula: C17H17F2NO3

Molecular Weight: 321.3185864


Assay: ≥99%

Packing: Export worthy packing

Material Safety Data Sheet: Available on request

Usage :

Ticagrelor is a reversible antagonist of the platelet purinergic P2Y12 receptor, which is the main receptor responsible for ADP-induced platelet aggregation.

Related intermediate:

1) 274693-27-5 Ticagrelor

2) 4,6-Dichloro-5-nitro-2-(propylthio)pyrimidine 145783-14-8

3) 4,6-Dichloro-2-propylthiopyrimidine-5-amine 145783-15-9

4) (1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine L-Tartaric acid 220352-39-6

5) 1156491-10-9, (1R trans)-2-(3,4-difluorophenyl)cyclopropane amine

6) 376608-74-1, Ethanol,2-[[(3aR,4S,6R,6aS)-6-[[5-aMino-6-chloro-2-(propylthio)-4-pyriMidinyl]aMino]tetrahydro-2,2-diMethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]-

7) 376608-71-8, (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine (2R)-Hydroxy(phenyl)ethanoate

8) 376608-65-0, 2-((3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yloxy)ethanol L-tataric acid

Ticagrelor Impurities:

1)2-((3aS,4R,6S,6aR)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yloxy)ethanol (2S,3S)-2,3-dihydroxysuccinate

2) (1R,2R,3S,5R)-3-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
3) (1R,2R,3S,5R)-3-(7-(((1S,2R)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
4) (1S,2S,3R,5S)-3-(7-(((1S,2R)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol

Taizhou Volsen Chemical Co., Ltd.


Taizhou Volsen Chemical Co., Ltd. is professional in R&D, producing and marketing Pharmaceutical raw materials, pharmaceutical intermediates in China. VOLSEN consists of about 100 experienced employees including 3 PhD and 10 Master, and 35000 sqm facilities including research laboratories, kilo lab, pilot plant and full manufacturing plant,

VOLSEN R&D specialists, quality manager and sales with abundance experience make sure products are reliable and service is professional. The producing person inspect every step of the whole process and check up the quality strictly, in order to insure every batch of raw material achieve the standard of EP,CP, JP,BP etc.Matching to the diversified requirements of companies VOLSEN is steadily marching to reach the peaks.

Volsen owns a professional custom synthesis department, with more than 15 senior scientific research chemical personnels who have a graduate degree or above. We also have an independent scientific management system. Our company integrates years of production experiences and talent reserves that forms a strong R&D production capacity, furthermore we could undertake various chemicals customizations from kg to ton relying on the existing production base and equipment.

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Company Info

  • Company Name: Taizhou Volsen Chemical Co., Ltd.
  • Representative: Mr Chen
  • Product/Service: Favipiravir Intermediates , Arbidol Intermediates , Relugolix Intermediates , Vilanterol Intermediates , Remdesivir Intermediates , Umeclidinium Bromide
  • Capital (Million US $): 60000000RMB
  • Year Established: 2002
  • Total Annual Sales Volume (Million US $): Above US$100 Million
  • Export Percentage: 91% - 100%
  • Total Annual Purchase Volume (Million US $): Below US$1 Million
  • No. of Production Lines: 5
  • No. of R&D Staff: 91 -100 People
  • No. of QC Staff: 11 -20 People
  • OEM Services Provided: yes
  • Factory Size (Sq.meters): 30,000-50,000 square meters
  • Factory Location: Dongying Economic Development Zone , Dongying, Shandong,China
  • Contact Person: Ms. Amy Cheng
  • Tel: 86-576-88869393
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