900161-11-7

Usage

Uses

Used in Cardiovascular Medicine:
Vorapaxar sulfate M-9 is used as an antiplatelet agent for preventing blood clot formation in patients with a history of myocardial infarction or peripheral arterial disease. It works by inhibiting the binding of thrombin to PAR-1, thereby reducing platelet activation and aggregation.
Used in Reducing Cardiovascular Events:
Vorapaxar sulfate M-9 is used as a therapeutic option for reducing the risk of cardiovascular events, such as heart attack and stroke, in clinical trials. It has shown efficacy in managing cardiovascular diseases.
Caution:
Vorapaxar sulfate M-9 should be used with caution in patients at risk of bleeding complications.

Upstream product

• 541-41-3 chloroformic acid ethyl ester 
• 899809-64-4 3-(5-nitro-cyclohex-1-enyl)-acrylic acid 
• 899809-61-1 (R,Z)-4-hydroxy-N,N-diphenylpent-2-ynamide 
• 900161-09-3 (R,E)-3-(5-((ethoxycarbonyl)amino)cyclohex-1-en-1-yl)acrylic acid 

Downstream Products

• 900161-12-8 C₂₉H₃₄N₂O₅ 

Relevant academic research and scientific papers

Vorapaxar intermediate and preparation method thereof

The invention relates to an anticoagulant vorapaxar intermediate compound and a preparation method thereof. The preparation method specifically comprises that a completely-new oxime-based compound B is used as a starting compound, a five-step reaction is performed to synthesize the key amide intermediate G of vorapaxar, and through the intermediate, vorapaxar and the analog thereof can be furtherconveniently synthesized. According to the present invention, the use of the high-polarity and high-boiling-point solvent is avoided, the too-low-temperature operation and the too-high-temperature operation are avoided, and the method has characteristics of simpleness, easy performing and low production cost, and is suitable for industrial production. The specific route is defined in the specification.

Preparation method of vorapaxar intermediate

The invention belongs to the field of organic synthesis and drug synthesis, and relates to a preparation method of a vorapaxar intermediate. The preparation method comprises following steps: racemic (E)-3-(5-amino cyclohexyl-1-ene-yl) acrylic acid or an ester compound of (E)-3-(5-amino cyclohexyl-1-ene-yl) acrylic acid is reacted with D-malic acid so as to obtain optically pure (R, E)-3-(5-amino cyclohexyl-1-ene-yl) acrylic acid or a D-malate of the ester compound of (E)-3-(5-amino cyclohexyl-1-ene-yl) acrylic acid via resolution, and the obtained product is converted into (R,E)-3-(5-((ethoxycarbonyl)amino) cyclohexyl-1-ene-1-yl) acrylic acid; and at last the intermediate is converted into a subsequent intermediate of vorapaxar. Compared with the prior art, the preparation method possessesfollowing advantages: the yield is increased obviously, the raw materials are easily available; the production cost is low; the preparation method is simple; operation is convenient; the reaction reagents are friendly to the environment; the preparation method is better than the prior art, and is especially suitable for industrialized production.

Vorapaxar intermediate and preparation method thereof

The invention discloses a vorapaxar intermediate and a preparation method thereof. The invention provides the preparation method of the vorapaxar intermediate I, wherein the preparation method comprises the following steps: in a closed system, and under c

AN EXO-SELECTIVE SYNTHESIS OF HIMBACINE ANALOGS

This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the ch