Process for preparation of optically active sulfonamides and intermediates for their synthesis
    11.
    发明授权
    Process for preparation of optically active sulfonamides and intermediates for their synthesis 有权
    制备光学活性磺酰胺及其合成中间体的方法

    公开(公告)号:US06982344B2

    公开(公告)日:2006-01-03

    申请号:US10399165

    申请日:2001-10-17

    摘要: A method including resolution of a diastereomeric mixture represented by the formula wherein R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, only one of R1 and R2 contains one asymmetric carbon, and Ra is an optically active and optionally substituted hydrocarbon group or an optically active and optionally substituted heterocyclic group, or a salt thereof, to produce the diastereomer having a steric configuration of the asymmetric carbon for R1 or R2 of an R configuration or an S configuration, or a salt thereof.

    摘要翻译: 一种包括由下式表示的非对映异构体混合物的拆分方法,其中R 1和R 2相同或不同,并且各自为任选取代的烃基或任选取代的杂环 基团中,R 1和R 2中只有一个含有一个不对称碳,R a是光学活性和任选取代的烃基或 光学活性和任选取代的杂环基或其盐,以产生R构型的R 1或R 2的不对称碳的立体构型的非对映异构体或 S构型或其盐。

    Process for producing cyclic compound
    13.
    发明授权
    Process for producing cyclic compound 失效
    环状化合物的制备方法

    公开(公告)号:US07038042B2

    公开(公告)日:2006-05-02

    申请号:US11010215

    申请日:2004-12-10

    IPC分类号: C07D487/00 C07C313/00

    摘要: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2-Z is not —X1—X2—CH2, -Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.

    摘要翻译: 一种适用于通过短步安全批量生产用于药物,农药,食品,化妆品和化学产品的环状化合物或其中间体的方法。 该方法用于制备由下式表示的化合物:其中Z表示吸电子基团; W表示任选取代的乙烯或任选取代的亚乙烯基; R 3表示氢或任选取代的烃基; 并且X表示二价基团[条件是当W表示任选取代的亚乙烯基时,则-X-CH 2 -Z不是-X 1 - 2 - -CH 2 - ,其中X 1表示硫或任选取代的氮,X 2表示任选取代的亚乙基)]} 或其盐的特征在于,在含有碳酸二酯的溶剂中使式(II)表示的化合物或其盐(其中符号具有与上述相同的含义)进行闭环反应。

    Processes for the preparation of 2,3-dihydrothiepine derivatives
    14.
    发明授权
    Processes for the preparation of 2,3-dihydrothiepine derivatives 失效
    2,3-二氢硫嘌呤衍生物的制备方法

    公开(公告)号:US06566535B1

    公开(公告)日:2003-05-20

    申请号:US10019987

    申请日:2001-11-07

    IPC分类号: C07D33712

    CPC分类号: C07D337/08 C07D337/04

    摘要: A process for preparing a compound represented by the following formula: wherein each symbol is as defined below, or a salt thereof, characterized by subjecting a compound represented by the following formula: wherein R1 is an electron-attracting group; R2, R3, R4, R5, R6 and R7 are each a hydrogen atom, a halogen atom, an optionally substituted amino group, an optionally substituted hydroxyl group, an optionally substituted thiol group, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group, provided that R6 and R7 may be united to form a ring; and R8 is a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, to a ring-closing reaction.

    摘要翻译: 一种制备由下式表示的化合物的方法:其中每个符号如下所定义,或其盐,其特征在于使下式表示的化合物:其中R1是吸电子基团; R2,R3,R4,R5,R6和R7各自为氢原子,卤素原子,任选取代的氨基,任选取代的羟基,任选取代的硫醇基,任选取代的烃基或任选取代的杂环 组合,条件是R 6和R 7可以结合形成环; 并且R8是氢原子或任选取代的烃基或其盐进行闭环反应。

    Cephem compounds, their production and use
    15.
    发明授权
    Cephem compounds, their production and use 失效
    头孢烯化合物,其生产和使用

    公开(公告)号:US4921851A

    公开(公告)日:1990-05-01

    申请号:US396758

    申请日:1989-08-22

    摘要: This invention relates to a compound of the formula: ##STR1## wherein Q is nitrogen or CH; R.sup.1 is hydrogen or a lower alkyl group which may be substituted; and ring A is a pyridine or pyridazine ring which is substituted at the ring-constituting carbon atom by a group of the formula:--E--(CH.sub.2).sub.n --R.sup.2in which E is sulfur or NH; R.sup.2 is an amino, carbamoylamino, formylamino, acetylamino, N-formimidoylamino, N-acetimidoylamino, lower alkylamino, hydroxyl or carbamoyloxy group; and n is an integer of 2 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) or a pharmaceutically acceptable sale thereof has excellent antibacterial activity and is used as antibiotics.

    摘要翻译: 本发明涉及下式的化合物:其中Q是氮或CH; R1是氢或可被取代的低级烷基; 环A为吡啶或哒嗪环,其在环的构成碳原子上被下列基团取代:其中E为硫或NH的-E-(CH2)n-R2; R2是氨基,氨基甲酰基氨基,甲酰氨基,乙酰氨基,N-甲脒基氨基,N-亚氨代乙酰氨基,低级烷基氨基,羟基或氨基甲酰氧基; n为2〜4的整数,或其药学上可接受的盐。 化合物(I)或其药学上可接受的销售具有优异的抗菌活性并用作抗生素。

    Cephem compounds
    17.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号:US4833134A

    公开(公告)日:1989-05-23

    申请号:US84882

    申请日:1987-08-13

    CPC分类号: C07D501/46

    摘要: Cephem compounds of the formula: ##STR1## wherein Q stands for a nitrogen atom or CH, R.sup.1 stands for a hydrogen atom or an optionally substituted lower alkyl group, R.sup.2 stands for a hydrogen atom or a lower alkyl group, A stands for a sulfur atom or NH, and n denotes an integral number ranging from 2 to 4, or salts thereof, and processes for producing them. The compounds (I) or salts thereof show not only excellent antibacterial activities against a wide range of pathogenic bacteria from gram-positive to gram-negative ones, including a variety of strains isolated clinically but also hydrophilic properties, and therefore they are excellent antibiotic substances having desirable water-solubility when used as injections.

    摘要翻译: 下式的头孢烯化合物:其中Q代表氮原子或CH,R1代表氢原子或任选取代的低级烷基,R2代表氢原子或低级烷基 A表示硫原子或NH,n表示2〜4的整数,或其盐,及其制造方法。 化合物(I)或其盐不仅具有针对从革兰氏阳性至革兰氏阴性菌的广泛病原菌的优良抗菌活性,包括临床分离的各种菌株,而且亲水性,因此它们是优异的抗生素物质 当用作注射剂时具有所需的水溶性。

    Process for producing cyclic compound
    18.
    发明申请
    Process for producing cyclic compound 失效
    环状化合物的制备方法

    公开(公告)号:US20050096475A1

    公开(公告)日:2005-05-05

    申请号:US11010215

    申请日:2004-12-10

    摘要: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2-Z is not —X1—X2—CH, -Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.

    摘要翻译: 一种适用于通过短步安全批量生产用于药物,农药,食品,化妆品和化学产品的环状化合物或其中间体的方法。 该方法用于制备由下式表示的化合物:其中Z表示吸电子基团; W表示任选取代的乙烯或任选取代的亚乙烯基; R 3表示氢或任选取代的烃基; 并且X表示二价基团[条件是当W表示任选取代的亚乙烯基时,则-X-CH 2 -Z不为-X 1 -X 2 - 其中X 1表示硫或任选取代的氮,X 2表示任选取代的乙烯)]}或其盐,其特征在于: 将含有式(II)的化合物或其盐(其中符号具有与上述相同的含义)与含有碳酸二酯的溶剂进行闭环反应。

    Process for producing cyclic compound
    19.
    发明授权
    Process for producing cyclic compound 失效
    环状化合物的制备方法

    公开(公告)号:US06864367B2

    公开(公告)日:2005-03-08

    申请号:US10204315

    申请日:2001-02-20

    摘要: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2—Z is not —X1—X2—CH2—Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.

    摘要翻译: 一种适用于通过短步安全批量生产用于药物,农药,食品,化妆品和化学产品的环状化合物或其中间体的方法。 该方法用于制备由下式表示的化合物:其中Z表示吸电子基团; W表示任选取代的乙烯或任选取代的亚乙烯基; R 3表示氢或任选取代的烃基; 并且X表示二价基团[条件是当W表示任选取代的亚乙烯基时,则-X-CH 2 -Z不是-X 1 -X 2 -CH 2 -Z(其中X 1表示硫或任选取代的 氮和X 2表示任选取代的乙烯)]}或其盐,其特征在于将式(II)表示的化合物或其盐:(其中符号具有与上述相同的含义) 在含有碳酸二酯的溶剂中进行闭环反应。