900161-12-8Relevant articles and documents
Preparation method of vorapaxar intermediate
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, (2018/02/24)
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.
HIGH PURITY SYNTHETIC PROCESS FOR THE PREPARATION OF DODECAHYDRO-NAPTHO-FURANYL-CARBAMIC ACID ESTER INTERMEDIATES
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Page/Page column 13-19, (2009/05/30)
This application discloses a novel process to synthesize himbacine analog compounds, and intermediates of formula (I) useful in the synthesis thereof. The subject compounds are useful as Thrombin Receptor Antagonists with useful pharmaceutical properties.