900161-09-3Relevant 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.
AN EXO-SELECTIVE SYNTHESIS OF HIMBACINE ANALOGS
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Page/Page column 40; 41, (2008/06/13)
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
