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    Tertiary-butyldimethylsilyl carbamate derivative and process for producing the same
    3.
    发明授权
    Tertiary-butyldimethylsilyl carbamate derivative and process for producing the same 失效
    叔丁基二甲基甲硅烷基氨基甲酸酯衍生物及其制备方法

    公开(公告)号：US4837349A

    公开(公告)日：1989-06-06

    申请号：US909397

    申请日：1986-09-19

    申请人： Yasufumi Ohfune ,  Masahiro Sakaitani

    发明人： Yasufumi Ohfune ,  Masahiro Sakaitani

    IPC分类号： C07F7/18

    CPC分类号： C07F7/1896

    摘要： A t-butyldimethylsilyl carbamate derivative and a process for producing the same are disclosed. Tertiary-butyldimethylsilyl carbamate derivatives having the following general formula (1) are intermediates for the production of a variety of carbamate esters that can be extensively used as drugs acting on the central nervous system or circulatory organs, as agrichemicals (e.g. insecticides and herbicides), or as antimicrobial agents; a process capable of economical and efficient production of such intermediates is also disclosed: ##STR1## where R.sup.1 is an alkyl group having 1-3 carbon atoms or a hydrogen atom; R.sup.2 is ##STR2## (where R.sup.3 is a hydrogen atom, an alkyl, alkenyl or aralkyl group having 1-10 carbon atoms, each of which groups may be substituted by a hydroxyl group, a t-butyldimethylsilyloxy group, a methylthio group, a lower alkoxycarbonyl group, a lower alkoxy group, an indolyl group or an imidazolyl group; R.sup.4 is a lower alkoxycarbonyl group, an N-alkylamido group having 2-6 carbon atoms, an O-tetrahydropyranylthr eonine methyl ester amido residue, an O-t-butyldimethylsilylthreonine methyl ester amido residue, a threonine methyl ester amido residue or --(CH.sub.2).sub.n --COOR.sup.5 (where n is an integer of 1-3 and R.sup.5 is a lower alkyl group), provided that R.sup.3 combines with R.sup.4 to form a cyclopentyl group, a cyclohexyl group, a tetrahydrofuranyl group or a dioxanyl group, these rings being optionally substituted by a lower alkyl group, a lower alkenyl group, a lower alkoxycarbonyl group or a lower alkoxycarbonylmethyl group); and R.sup.1 and R.sup.2, when taken together, form a 4- or 5-membered carbon ring, which may be substituted by a lower alkoxycarbonyl group or a t-butyldimethylsilyloxycarbonyl group.

    摘要翻译： 公开了一种叔丁基二甲基甲硅烷基氨基甲酸酯衍生物及其制备方法。 具有以下通式（1）的叔丁基二甲基甲硅烷基氨基甲酸酯衍生物是用于生产可广泛用作作为农药（例如杀虫剂和除草剂）作为中枢神经系统或循环器官的药物的各种氨基甲酸酯的中间体， 或作为抗微生物剂; 还公开了能够经济有效地生产这样的中间体的方法：其中R1是具有1-3个碳原子的烷基或氢原子的（1） R2是（其中R3是氢原子，具有1-10个碳原子的烷基，烯基或芳烷基，它们各自可以被羟基取代，叔丁基二甲基甲硅烷氧基，甲硫基， 低级烷氧基羰基，低级烷氧基，吲哚基或咪唑基; R4为低级烷氧基羰基，具有2-6个碳原子的N-烷基酰氨基，O-四氢吡喃基硫代氨基甲酸酯酰胺残基，二叔丁基二甲基甲硅烷基苏氨酸 甲基酯酰氨基残基，苏氨酸甲酯酰氨基残基或 - （CH 2）n -COOR 5（其中n为1-3的整数，R 5为低级烷基），条件是R 3与R 4结合形成环戊基， 环己基，四氢呋喃基或二恶烷基，这些环任选被低级烷基，低级烯基，低级烷氧基羰基或低级烷氧基羰基甲基取代）。 当R 1和R 2一起形成可被低级烷氧基羰基或叔丁基二甲基甲硅烷氧基羰基取代的4-或5-元碳环时，

    2-(2,3-dicarboxycyclopropyl) glycine and method for producing the same
    4.
    发明授权
    2-(2,3-dicarboxycyclopropyl) glycine and method for producing the same 失效
    2-（2,3-二羧基环丙基）甘氨酸及其制备方法

    公开(公告)号：US5334757A

    公开(公告)日：1994-08-02

    申请号：US53693

    申请日：1993-04-29

    申请人： Yasufumi Ohfune ,  Keiko Shimamoto ,  Haruhiko Shinozaki ,  Michiko Ishida

    发明人： Yasufumi Ohfune ,  Keiko Shimamoto ,  Haruhiko Shinozaki ,  Michiko Ishida

    IPC分类号： A61K31/195 ,  A61P25/00 ,  A61P25/08 ,  C07C227/18 ,  C07C229/46

    CPC分类号： C07C229/46 ,  C07C2101/02

    摘要： (2S,1'R,2'R,3'R)-2-(2,3-dicarboxycyclopropyl)-glycine (DCG-I) and (2S,1'S,2'S,3'S)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-II), as well as methods for synthesizing these compounds are provided. Studies on L-glutamate receptors with the use of DCG-I and DCG-II, which are agonists for NMDA receptors, contribute to the development of remedies for various nervous disorders. Further, DCG-I and DCG-II selectively inhibit monosynaptic reflex even at a low concentration, which makes them useful as a remedy for spastic palsy, an anesthetic and an analgesic.

    摘要翻译： （2S，1'R，2'R，3'R）-2-（2,3-二羧基环丙基） - 甘氨酸（DCG-1）和（2S，1'S，2'S，3'S） 二羧基环丙基）甘氨酸（DCG-II），以及合成这些化合物的方法。 使用作为NMDA受体激动剂的DCG-1和DCG-II对L-谷氨酸受体的研究有助于各种神经障碍的治疗的发展。 此外，即使在低浓度下，DCG-I和DCG-II选择性地抑制单突触反射，这使得它们可用作痉挛性麻痹，麻醉剂和止痛剂的补救剂。

    Mass spectrometric method for structural analysis of chain nitrogen-containing compounds using sqauric acid
    6.
    发明授权
    Mass spectrometric method for structural analysis of chain nitrogen-containing compounds using sqauric acid 失效
    使用平sq酸对链状含氮化合物进行结构分析的质谱法

    公开(公告)号：US07560286B2

    公开(公告)日：2009-07-14

    申请号：US10095017

    申请日：2002-03-12

    申请人： Hideo Naoki ,  Terumi Nakajima ,  Yasufumi Ohfune ,  Tetsuro Shinada ,  Kazuya Murata

    发明人： Hideo Naoki ,  Terumi Nakajima ,  Yasufumi Ohfune ,  Tetsuro Shinada ,  Kazuya Murata

    IPC分类号： G01N24/00

    CPC分类号： C07C49/753 ,  C07C45/70 ,  Y10T436/17 ,  Y10T436/24

    摘要： A method for effectively causing charge-remote fragmentation (CRF) when the structural analysis of an nitrogen-containing organic compound is performed using a high-energy collisional-induced dissociation-mass/mass spectrum (CID-MS/MS spectrum), a reagent to be used in such a method, and a method for analyzing an organic compound by the induction of CRF are provided. The method for the induction of charge-remote fragmentation (CRF) using a high-energy collisional-induced dissociation-mass/mass spectrum (CID-MS/MS spectrum) has the step of: introducing a squaric acid residue into an end of a nitrogen-containing organic compound. The squaric acid residue is represented by a chemical formula (I): The reagent is provided for introducing such a squaric acid residue. Furthermore, the method is provided for analyzing such an organic compound by the induction of CRF.

    摘要翻译： 当使用高能碰撞诱导的解离质谱/质谱（CID-MS / MS谱）进行含氮有机化合物的结构分析时，有效地引起电荷远程碎片化（CRF）的方法， 用于这种方法，并且提供了通过诱导CRF分析有机化合物的方法。 使用高能碰撞诱导的解离 - 质谱/质谱（CID-MS / MS谱）诱导电荷远程碎裂（CRF）的方法具有以下步骤：将方酸残渣引入到 含氮有机化合物。 方酸残基由化学式（I）表示：提供用于引入方酸残基的试剂。 此外，提供了通过诱导CRF分析这种有机化合物的方法。