公开(公告)号：US07741473B2

公开(公告)日：2010-06-22

申请号：US11393374

申请日：2006-03-30

申请人： Paul S. Watson ,  James G. Douglass, III ,  Bob Suchozak ,  Subramanian Pandiaraju ,  Craig E. Dixon ,  Daniel Levin

发明人： Paul S. Watson ,  James G. Douglass, III ,  Bob Suchozak ,  Subramanian Pandiaraju ,  Craig E. Dixon ,  Daniel Levin

IPC分类号： C07H19/067 ,  C07H19/167

CPC分类号： C07F9/6561 ,  C07F9/65616 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

摘要： The present invention is directed to a processes for the synthesis of trans isomer of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles (Formula I). The process comprises the steps of: (a) obtaining a compound of Formula II, which is a mixture of cis and trans-diastereomers, and (b) chemically decomposing the compound of Formula II in a solution comprising a solvent and an acid that is a hydrogen donor or an electron pair acceptor, whereby the cis diastereomer is decomposed and the compound of Formula I is obtained. The compounds prepared by the present invention are useful in treating diseases or conditions associated with platelet aggregation and/or platelet activation.

摘要翻译： 本发明涉及合成4,6-二取代 - 四氢 - 呋喃，噻吩并，吡咯并环戊烷并[3,4] [1,3]二氧杂环戊烯（式I）的反式异构体的方法。 该方法包括以下步骤：（a）获得式II化合物，其是顺式和反式 - 非对映异构体的混合物，和（b）在包含溶剂和酸的溶液中化学分解式II化合物， 氢供体或电子对受体，由此使顺式非对映异构体分解并得到式I化合物。 通过本发明制备的化合物可用于治疗与血小板聚集和/或血小板活化相关的疾病或病症。