公开(公告)号：US6080878A

公开(公告)日：2000-06-27

申请号：US67903

申请日：1998-04-29

申请人： Maria de los Angeles Rey ,  Antonio Mourino ,  Ana Fernandez-Gacio ,  Yagamare Fall ,  Sebastianus J. Halkes ,  Koen M. Halkes ,  Jan-Paul van de Velde ,  Jan Zorgdrager

发明人： Maria de los Angeles Rey ,  Antonio Mourino ,  Ana Fernandez-Gacio ,  Yagamare Fall ,  Sebastianus J. Halkes ,  Koen M. Halkes ,  Jan-Paul van de Velde ,  Jan Zorgdrager

IPC分类号： A61K31/59 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07C35/27 ,  C07C49/665 ,  C07C401/00

CPC分类号： C07C401/00 ,  C07C59/90 ,  C07F7/1892 ,  C07C2102/24 ,  Y02P20/55

摘要： The invention relates to a new method of preparing 16-dehydro vitamin D compounds having formula I ##STR1## wherein: R has the epi-configuration or the normal configuration and represents straight or branched C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.3-6 -cycloalkyl, or an aromatic group optionally substituted with halogen, C.sub.1-3 -alkyl or alkoxy,Z is a saturated or unsaturated straight hydrocarbon group or oxahydrocarbon group containing 3-6 C-atoms which may be substituted with OH, F, alkyl (C.sub.1-3) or cycloalkyl (C.sub.3-5),R.sub.1 is hydrogen or an hydroxy protecting group,R.sub.2 is hydrogen or hydroxy, andA and B represent hydrogen or methyl, or together form the methylene group, to the new compounds having this formula and to new intermediates obtainable according to this process.

摘要翻译： 本发明涉及一种制备具有式I的16-脱氢维生素D化合物的新方法，其中：R具有外延构型或正构构型，并表示直链或支链C 1-6 - 烷基，C 2-6 - 烯基，C 3-6 环烷基或任选被卤素，C 1-3 - 烷基或烷氧基取代的芳基，Z是含有3-6个C原子的饱和或不饱和直链烃基或氧杂烃基，其可以被OH，F，烷基（ C 1-3）或环烷基（C 3-5），R 1是氢或羟基保护基，R 2是氢或羟基，A和B代表氢或甲基，或一起形成亚甲基， 以及根据该方法可获得的新中间体。