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    • 4. 发明申请
    • Method for Producing Fluorinated Proline Derivative
    • 生产氟化脯氨酸衍生物的方法
    • US20080114053A1
    • 2008-05-15
    • US11795961
    • 2006-01-26
    • Hidetoshi TsunodaTsuneji Suzuki
    • Hidetoshi TsunodaTsuneji Suzuki
    • A61K31/401
    • C07D207/16C07D207/22
    • An object of the present invention is to provide a method for efficiently producing a high-purity fluorinated proline derivative with high yield. A method for producing a compound represented by the general formula (2), (In the formula, R1 represents an unsubstituted or substituted alkyl group having 1 to 6 carbon atoms or the like, and R2 represents an unsubstituted or substituted alkyl group having 1 to 6 carbon atoms or the like, and R3 represents a hydroxyl group or the like) wherein a compound represented by the general formula (1) (In the formula, R1 and R2 are defined as in the general formula (1)) is reacted with a fluorination agent to obtain a reaction product containing the compound represented by the general formula (2) and a by-products; and bringing chlorine, bromine, iodine, hypochlorous acid, hypochlorite, hypobromous acid, hypobromite or N-halogenosuccinimide into action on the reaction product to chemically change the by-product.
    • 本发明的目的是提供一种以高产率有效地制备高纯度氟化脯氨酸衍生物的方法。 一种制备由通式(2)表示的化合物的方法,(式中,R 1表示未取代或取代的碳原子数为1〜6的烷基等,R 2表示未取代或取代的烷基, 6个碳原子等,R3表示羟基等),其中由通式(1)表示的化合物(式中,R1和R2如通式(1)所定义)与式 得到含有通式(2)表示的化合物和副产物的反应产物的氟化剂; 并使氯,溴,碘,次氯酸,次氯酸盐,次溴酸,次溴酸盐或N-卤代琥珀酰亚胺作用于反应产物以化学改变副产物。
    • 5. 发明授权
    • Optically active azole derivative and process for producing the same
    • 光学活性唑衍生物及其制备方法
    • US07271185B2
    • 2007-09-18
    • US10503469
    • 2003-02-07
    • Tsuneji SuzukiHidetoshi Tsunoda
    • Tsuneji SuzukiHidetoshi Tsunoda
    • A61K31/41C07D249/04C07D249/08
    • C07D233/56C07D231/12C07D233/54C07D249/08Y02P20/55
    • A method for producing an optically active 2-phenyl-2,3,-dihydroxypropyl azole derivative, which is a useful compound in various fields. An optically active α-hydroxycarboxylic acid derivative represented by general formula (1) is used as a starting material and is allowed to react with an azole acetic acid derivative (2) to produce a new, optically active azole-alkyl ketone derivative (3). Subsequently, a new, optically active azole-methyl alcohol derivative (5) is produced by highly diastereoselective alkylation by an appropriate combination of a protective group and an organometallic reagent (4). Furthermore, the optically active azole-methyl alcohol derivative (5) is selectively deprotected to produce an optically active 2-phenyl-2,3-dihydroxypropyl azole derivative (6)
    • 光学活性的2-苯基-2,3-二羟基丙基唑衍生物的制造方法,其为各种领域的有用化合物。 使用由通式(1)表示的光学活性α-羟基羧酸衍生物作为原料,并与唑类乙酸衍生物(2)反应,生成新的光学活性唑 - 烷基酮衍生物(3) 。 随后,通过保护基和有机金属试剂(4)的适当组合,通过高度非对映选择性烷基化产生新的光学活性唑 - 甲醇衍生物(5)。 此外,光学活性的唑 - 甲醇衍生物(5)选择性脱保护,得到光学活性的2-苯基-2,3-二羟基丙基唑衍生物(6)