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    • 1. 发明授权
    • Method of optically resolving racemic alcohols with a bicyclooxaoctane or a bicycooxaoctene resolving reagents
    • 用双环氧辛烷或二氧杂辛烷拆分试剂旋光拆分外消旋醇的方法
    • US07674614B2
    • 2010-03-09
    • US11683322
    • 2007-03-07
    • Hisao NemotoMasayuki Shibuya
    • Hisao NemotoMasayuki Shibuya
    • C12P41/00
    • C07D307/935C07B2200/07C12C11/02Y10T436/204165
    • An optical resolving reagent comprising at least one of compounds represented by the following formulae (1) and (2) (1) (2) (wherein R1 to R8 each represents hydrogen or C1-20 alkyl; R9 represents optionally substituted C1-20 alkyl, optionally substituted C1-20 alkenyl, formyl, or acyl; and R10 represents C1-6 alkyl; provided that the molecule represented by the formula (1) is of the cis configuration with respect to R9 and OR10); and a method of optically resolving with the optical resolving reagent an alcohol having an asymmetric carbon atom in the molecule and represented by the formula (3): (R11)(R12)(R13)COH (wherein R11, R12, and R13 each represents hydrogen or optionally substituted C1-20 alkyl, provided that at least one of R11, R12, and R13 is not hydrogen). The method of optical resolution is highly suitable for general purposes. By the method, a mixture of optical isomers of any of various alcohols can be optically resolved easily and industrially advantageously.
    • 包含由下式(1)和(2)(1)(2)表示的化合物中的至少一种的光学拆分试剂(其中R 1至R 8各自表示氢或C 1-20烷基; R 9表示任选取代的C 1-20烷基 ,任选取代的C 1-20烯基,甲酰基或酰基; R 10表示C 1-6烷基;条件是由式(1)表示的分子相对于R9和OR10为顺式构型; (3)表示的具有不对称碳原子的醇:(R11)(R12)(R13)COH(其中R11,R12和R13各自表示 氢或任选取代的C 1-20烷基,条件是R 11,R 12和R 13中的至少一个不是氢)。 光学分辨率的方法非常适合于一般用途。 通过该方法,可以容易且工业上有利地光学拆分各种醇的光学异构体的混合物。
    • 2. 发明申请
    • Agent For Optical Resolution, Process For Producing Optically Active Substance and 1,5-Substituted Bicyclo [3.3.0] -2-Oxaoctane Compound
    • 光学拆分剂,用于制备光学活性物质和1,5-取代的双环[3.3.0] -2-氧杂辛烷化合物
    • US20080287695A1
    • 2008-11-20
    • US10588994
    • 2005-02-18
    • Hisao Nemoto
    • Hisao Nemoto
    • C07D307/935
    • C07B57/00C07C45/294C07D307/935C07C49/697
    • An agent for optical resolution comprising a bicyclo[3.3.0]-2-oxaoctane compound represented by the formula [1], [2] or [3] a process for producing an optically active substance comprising obtaining a mixture of diastereomers by reaction of the agent with a mixture of optically active substances having active hydrogen atom, resolving the mixture of diastereomers into each diastereomer and obtaining an (R) optically active substance or an (S) optically active substance by decomposition of the diastereomer; and compounds represented by the above formulae in which R11 represents fluorenylmethyl group, fluorenylidenemethyl group, bis(4-cyclohexylphenyl)methyl group, 4-(9-phenanthryl)phenyl group, 4-(1-pyrenyl)phenyl group, 4-(5-acenaphthenyl)phenyl group or 4-(9-anthryl)phenyl group, are disclosed. A useful optically active substance having a very high purity can be produced efficiently by using the agent of the present invention.
    • 一种用于光学拆分的试剂,其包含由式[1],[2]或[3]表示的双环[3.3.0] -2-氧代辛烷化合物,其是制备光学活性物质的方法,包括通过 具有活性氢原子的光学活性物质的混合物的试剂,将非对映异构体的混合物分解成各个非对映异构体并通过分解非对映体得到(S)光学活性物质或(S)光学活性物质; 由上式表示的化合物,其中R 11表示芴基甲基,芴基亚甲基,双(4-环己基苯基)甲基,4-(9-菲基)苯基,4-(1-芘基) )苯基,4-(5-苊基)苯基或4-(9-蒽基)苯基。 通过使用本发明的试剂可以有效地制备具有非常高纯度的有用的光学活性物质。
    • 7. 发明授权
    • Compound modified with glycerol derivative
    • 用甘油衍生物修饰的化合物
    • US07696359B2
    • 2010-04-13
    • US10570623
    • 2004-09-03
    • Hisao NemotoMasahiro YamauchiHiroko KusanoYasuki KatoMotoo YamasakiToshiyuki Suzawa
    • Hisao NemotoMasahiro YamauchiHiroko KusanoYasuki KatoMotoo YamasakiToshiyuki Suzawa
    • C07D207/46C07F9/09
    • C07D207/452A61K47/00A61K47/54A61K47/6911B82Y5/00C07C323/60C07F9/10C07K5/0202
    • Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R-X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.
    • 本发明的目的是提供一种可用作生产药物载体等的表面改性剂或其盐的化合物; 包含该颗粒的细颗粒; 等等。 本发明提供一种化合物,其中选自由两亲物质和疏水性物质组成的组中的被改性物质用下式(1)表示的甘油衍生物进行改性:其中R表示残基 包括选自两亲物质和疏水性物质的待修饰物质的反应性基团或能够与被修饰物质结合的间隔基,其选自两亲物质 和疏水性物质,至RX或能够转化为反应性基团的基团; n表示3以上的整数, X表示可以直接或经由间隔基或其盐具有n数的以下结构的残基: 包含该颗粒的细颗粒; 等等。
    • 9. 发明申请
    • OPTICAL RESOLVER AND METHOD OF OPTICALLY RESOLVING ALCOHOL WITH THE SAME
    • 光学分辨率和光学解决醇的方法
    • US20070155994A1
    • 2007-07-05
    • US11683322
    • 2007-03-07
    • Hisao NEMOTOMasayuki Shibuya
    • Hisao NEMOTOMasayuki Shibuya
    • C07C29/74C07D307/87
    • C07D307/935C07B2200/07C12C11/02Y10T436/204165
    • An optical resolving reagent comprising at least one of compounds represented by the following formulae (1) and (2) (1) (2) (wherein R1 to R8 each represents hydrogen or C1-20 alkyl; R9 represents optionally substituted C1-20 alkyl, optionally substituted C1-20 alkenyl, formyl, or acyl; and R10 represents C1-6 alkyl; provided that the molecule represented by the formula (1) is of the cis configuration with respect to R9 and OR10); and a method of optically resolving with the optical resolving reagent an alcohol having an asymmetric carbon atom in the molecule and represented by the formula (3): (R11) (R12) (R13)COH (wherein R11, R12, and R13 each represents hydrogen or optionally substituted C1-20 alkyl, provided that at least one of R11, R12, and R13 is not hydrogen) The method of optical resolution is highly suitable for general purposes By the method, a mixture of optical isomers of any of various alcohols can be optically resolved easily and industrially advantageously.
    • 一种光学拆分试剂,其包含由下式(1)和(2)(1)(2)表示的化合物中的至少一种(其中R 1〜R 8各自独立地 表示氢或C 1-20烷基; R 9表示任选取代的C 1-20烷基,任选取代的C 1-20 烯基,甲酰基或酰基; R 10表示C 1-6烷基;条件是由式(1)表示的分子是顺式 相对于R 9和OR 10的构型); 以及用光学拆分试剂在分子中具有不对称碳原子的醇进行光学拆分的方法,由式(3)代表:(R 11)(R 12) )(R 13)COH(其中R 11,R 12和R 12各自表示氢或 任选取代的C 1-12烷基,条件是R 11,R 12和R 13中的至少一个 >不是氢)光学拆分的方法非常适合于一般目的通过该方法,各种醇中的任何一种的光学异构体的混合物可以容易且工业上有利地光学拆分。