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    • 7. 发明申请
    • Benzamidine derivatives and process for production thereof
    • 苄脒衍生物及其制备方法
    • US20050101675A1
    • 2005-05-12
    • US10470382
    • 2002-01-28
    • Takayuki HaraToru MinoshimaMasayasu Tabe
    • Takayuki HaraToru MinoshimaMasayasu Tabe
    • C07C257/18C07D211/26A61K31/155
    • C07C257/18C07D211/26
    • A process for production of an amidine derivative represented by the following Formula (II) [wherein, R represents a hydrogen atom, an unsubstituted or substituted phenyl group, an unsubstituted or substituted C1-C10 alkyl group, an unsubstituted or substituted C1-C10 alkoxy group, an unsubstituted or substituted C1-C10 alkoxycarbonyl group, or a hydroxyl group present at the ortho, meta, or para position] or a salt thereof, comprising the steps of reducing an amidoxime derivative represented by the following Formula (I) [wherein, R represents a hydrogen atom, an unsubstituted or substituted phenyl group, an unsubstituted or substituted C1-C10 alkyl group, an unsubstituted or substituted C1-C10 alkoxy group, an unsubstituted or substituted C1-C10 alkoxycarbonyl group, or a hydroxyl group present at the ortho, meta, or para position] with zinc in an acetic acid as a solvent.
    • 一种制备由下式(II)表示的脒衍生物的方法[其中,R表示氢原子,未取代或取代的苯基,未取代或取代的C1-C10烷基,未取代或取代的C1-C10烷氧基 基团,未取代或取代的C 1 -C 10烷氧基羰基,或邻位,间位或对位存在的羟基]或其盐,包括以下步骤:还原由下式(I)表示的偕胺肟衍生物[其中 R表示氢原子,未取代或取代的苯基,未取代或取代的C1-C10烷基,未取代或取代的C1-C10烷氧基,未取代或取代的C1-C10烷氧基羰基或存在于 邻位,间位或对位]与锌在乙酸中作为溶剂。
    • 8. 发明授权
    • Intermediates for vitamin D and processes for the preparation thereof
    • 维生素D的中间体及其制备方法
    • US06753435B1
    • 2004-06-22
    • US10239778
    • 2002-09-25
    • Masahiro KogaToru Minoshima
    • Masahiro KogaToru Minoshima
    • C07C40100
    • C07C401/00C07C309/65C07C2601/14C07C2601/16C07C2602/24C07F7/1804C07F7/1892
    • An object of the present invention is to provide intermediates for the synthesis of 1&agr;-hydroxyvitamin D derivatives useful as drugs and processes for the preparation thereof. Namely, the present invention is a process for the preparation of a compound represented by the formula (2), which comprises reacting a compound represented by the formula (1) with a compound represented by the formula (4) in the presence of a palladium catalyst, a process for the preparation of a compound represented by the formula (3), which comprises further catalytically reducing the resulting compound represented by the formula (2) in the presence of a Lindlar catalyst and hydrogen gas and heating the obtained product and a process for the preparation of a compound represented by the formula (5), which comprises further oxidizing the resulting compound represented by the formula (3) with an oxidizing agent and the compounds represented by the formulae (1) to (3):
    • 本发明的目的是提供用作合成作为药物的1α-羟基维生素D衍生物的中间体及其制备方法。本发明是制备式(2)表示的化合物的方法, 其包括在钯催化剂存在下使式(1)表示的化合物与式(4)表示的化合物反应,制备由式(3)表示的化合物的方法,该方法还包括 在Lindlar催化剂和氢气的存在下催化还原由式(2)表示的化合物,并加热得到的产物和制备由式(5)表示的化合物的方法,该方法包括进一步氧化所得 由式(3)表示的化合物与氧化剂和由式(1)至(3)表示的化合物: