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A kind of method for preparing (1r,2s)-2-(3,4-difluorophenyl) cyclopropylamine

A technology of difluorophenyl and cyclopropylamine, applied in the field of preparation of (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine, which can solve the problem of unsatisfactory yield and purity, long synthetic route, etc. question

Active Publication Date: 2017-12-22
SHANGHAI SYNCORES TECH INC
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0014] The synthetic routes reported in the above prior art are relatively long, and the yield and purity are not ideal, and some of them need to use explosive dangerous goods, all of which limit the industrial production of the above methods

Method used

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  • A kind of method for preparing (1r,2s)-2-(3,4-difluorophenyl) cyclopropylamine
  • A kind of method for preparing (1r,2s)-2-(3,4-difluorophenyl) cyclopropylamine
  • A kind of method for preparing (1r,2s)-2-(3,4-difluorophenyl) cyclopropylamine

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Embodiment Construction

[0041] The following examples illustrate but do not limit the invention.

[0042] Synthetic and Analytical Method Information: All commercially available reagents were used without purification and solvents were not treated. Column chromatography separation uses 200-300 mesh silica gel. Melting points are uncorrected. NMR ( 1 H, 19 F) The nuclear magnetic resonance is detected on a Mercury® 400MHz nuclear magnetic resonance instrument, and the solvents are deuterated chloroform and deuterated dimethyl sulfoxide. Low-resolution mass spectrometry was performed on an Agilent® 1024 mass spectrometer using electrospray method (ESI). HPLC is carried out on Shimadzu (SHIMADZU) HPLC instrument, model is SIL-20A or Agilent® HPLC instrument, model is LC-20AD. Chiral HPLC was performed on an Agilent® HPLC instrument, model 1200.

[0043] step a : Preparation of 1-(3,4-difluorophenyl)ethanone:

[0044]

[0045] Anhydrous aluminum trichloride (117g) was added to a mixed solution...

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Abstract

The invention relates to a method for preparing formula I(1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine; the method uses 1-(3,4-difluorophenyl)ethylene as The raw materials are successively passed through the new compound formula IV and formula V to obtain the mixture of formula I; The key intermediate of anticoagulant ticagrelor; the method is safe, environment-friendly, low-cost, and suitable for large-scale production.

Description

technical field [0001] The invention relates to a preparation method and a salt of an anticoagulant ticagrelor key intermediate (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine. Background technique [0002] Ticagrelor, developed by AstraZeneca, was approved by the FDA on July 20, 2011 to reduce the occurrence of thrombotic events in patients with acute coronary syndrome (ACS). It is a new type of selective anticoagulant and the first reversible binding P 2 Y 12 An adenosine diphosphate receptor (ADP) antagonist that reversibly acts on the purine 2 receptor subtype P on vascular smooth muscle cells (VSMC) 2 Y 12 , has obvious inhibitory effect on platelet aggregation caused by ADP, and can effectively improve the symptoms of patients with acute coronary heart disease. [0003] In 2012, the trade name of ticagrelor (or ticagrelor), Bilinda, has obtained the import drug license issued by the State Food and Drug Administration (SFDA), which means that this medicine for acute ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C211/40C07C209/62C07C209/88C07C23/18
Inventor 姜秀召黄鲁宁顾虹
Owner SHANGHAI SYNCORES TECH INC
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