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    1-Oxadethiacepham compounds and process for producing said compounds
    1.
    发明授权
    1-Oxadethiacepham compounds and process for producing said compounds 失效
    1-氧杂十八胺化合物及其制备方法

    公开(公告)号：US4366316A

    公开(公告)日：1982-12-28

    申请号：US322662

    申请日：1981-11-18

    申请人： Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Teruji Tsuji ,  Wataru Nagata

    发明人： Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Teruji Tsuji ,  Wataru Nagata

    IPC分类号： C07D498/04 ,  C07D505/00

    CPC分类号： C07D505/00

    摘要： Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl group derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving group are prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid. The new compounds of this invention shown by the following formula: ##STR4## wherein A is amino or substituted amino;E is hydrogen or methoxy; andY is a divalent group of the following formula: ##STR5## in which COB, X, and Z are as defined above are convertible into other compounds of the same formula by applying conventional methods in .beta.-lactam chemistry.

    摘要翻译： 用于制备由下式表示的抗细菌1-脱氧-1-氧杂头孢菌素的中间体：其中R是衍生自羧酸或碳酸的酰基的一价基团（减去羰基）; Y1是下式的二价基团：其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z是离去基团由下式的化合物制备：其中R和Y1如上所定义，通过酸的作用。 本发明的新化合物由下式表示：其中A是氨基或取代的氨基; E是氢或甲氧基; 并且Y是下式的二价基团：其中COB，X和Z如上定义的可通过在β-内酰胺化学中应用常规方法转化为相同式的其它化合物。

    Oxazolines
    2.
    发明授权
    Oxazolines 失效
    恶唑啉

    公开(公告)号：US4220766A

    公开(公告)日：1980-09-02

    申请号：US868422

    申请日：1978-01-10

    申请人： Teruji Tsuji ,  Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Wataru Nagata

    发明人： Teruji Tsuji ,  Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Wataru Nagata

    IPC分类号： C07D498/04 ,  C07D499/00 ,  C07D505/00 ,  C07D285/16 ,  C07D491/04

    CPC分类号： C07D505/00 ,  C07D499/00 ,  Y02P20/582

    摘要： Useful intermediates for preparing a 1-dethia-1-oxacephalosporin and represented by the following formula: ##STR1## (wherein R is a monovalent group resulting from the elimination of the carbonyl function of an acyl group derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy; andX is hydrogen or a nucleophilic group)are prepared from the corresponding penicillin 1-oxides of the following formula: ##STR2## (wherein R, COB, and X are as defined above) by heating, if required in the presence of the desulfurizing reagent, or by exchanging the X group with another one under the condition of an appropriate nucleophilic substitution.

    摘要翻译： 用于制备1-脱硫-1-氧杂环孢菌素并由下式表示的有用的中间体：其中R是由消除衍生自羧酸或碳酸的酰基的羰基官能团产生的一价基团; COB 是羧基或被保护的羧基; X是氢或亲核基团）由相应的下式的青霉素1-氧化物制备：如果需要，通过加热，其中R，COB和X如上所定义 在脱硫试剂的存在下，或者通过在适当的亲核取代条件下与另一种X基团交换X基团。

    Oxazolines
    4.
    发明授权
    Oxazolines 失效
    恶唑啉

    公开(公告)号：US4271295A

    公开(公告)日：1981-06-02

    申请号：US112144

    申请日：1980-01-14

    申请人： Teruji Tsuji ,  Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Wataru Nagata

    发明人： Teruji Tsuji ,  Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Wataru Nagata

    IPC分类号： C07D498/04 ,  C07D499/00 ,  C07D505/00 ,  C07D401/14 ,  C07D413/14

    CPC分类号： C07D505/00 ,  C07D499/00 ,  Y02P20/582

    摘要： Useful intermediates for preparing a 1-dethia-1-oxacephalosporin and represented by the following formula: ##STR1## (wherein R is a monovalent group resulting from the elimination of the carbonyl function of an acyl group derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy; andX is hydrogen or a nucleophilic group)are prepared from the corresponding penicillin 1-oxides of the following formula: ##STR2## (wherein R, COB, and X are as defined above) by heating, if required in the presence of a desulfurizing reagent, or by exchanging the X group with another one under the condition of an appropriate nucleophilic substitution.

    摘要翻译： 用于制备1-脱硫-1-氧杂环孢菌素并由下式表示的有用的中间体：其中R是由消除衍生自羧酸或碳酸的酰基的羰基官能团产生的一价基团; COB 是羧基或被保护的羧基; X是氢或亲核基团）由相应的下式的青霉素1-氧化物制备：如果需要，通过加热，其中R，COB和X如上所定义 在脱硫试剂的存在下，或者通过在适当的亲核取代条件下将X基团与另一种基团交换。

    1-Oxadethiacepham compounds
    6.
    发明授权
    1-Oxadethiacepham compounds 失效
    1-氧杂十八胺化合物

    公开(公告)号：US4478997A

    公开(公告)日：1984-10-23

    申请号：US543664

    申请日：1983-10-19

    申请人： Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Teruji Tsuji ,  Wataru Nagata

    发明人： Mitsuru Yoshioka ,  Shoichiro Uyeo ,  Yoshio Hamashima ,  Ikuo Kikkawa ,  Teruji Tsuji ,  Wataru Nagata

    IPC分类号： C07D498/04 ,  C07D498/20 ,  C07D505/00

    CPC分类号： C07D505/00

    摘要： Intermediates for preparing an antibacterial 1-dethia-1-oxa-cephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving groupare prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid.

    摘要翻译： 用于制备由下式表示的抗菌1-脱氧-1-氧杂 - 头孢菌素的中间体：其中R是衍生自羧酸或碳酸的酰基的一价基团（减去羰基）; Y1是下式的二价基团：其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z是离去基团由下式的化合物制备：其中R和Y1如上所定义，通过酸的作用。

    Azetidinone derivatives and production thereof
    7.
    发明授权
    Azetidinone derivatives and production thereof 失效
    氮杂环丁酮衍生物及其制备

    公开(公告)号：US4233216A

    公开(公告)日：1980-11-11

    申请号：US967007

    申请日：1978-12-06

    申请人： Shoichiro Uyeo ,  Mitsuru Yoshioka ,  Teruji Tsuji ,  Ikuo Kikkawa ,  Wataru Nagata

    发明人： Shoichiro Uyeo ,  Mitsuru Yoshioka ,  Teruji Tsuji ,  Ikuo Kikkawa ,  Wataru Nagata

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07D505/00 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

    CPC分类号： C07D205/085 ,  C07D505/00

    摘要： .alpha.-[3(R)-Substituted amino-4(R)-substituted alkoxy-2-oxo-azetidin-1-yl]-.alpha.-isopropenylacetate (Ia) and .alpha.-[3(R)-substituted amino-4(R)-substituted alkoxy-2-oxo-azetidin-1-yl]-.alpha.-isopropylideneacetate (Ib) prepared from (1R,5S)-.alpha.-(3-substituted-7-oxo-4-oxa-2,6-diazabicyclo[3.2.0]hept-2-en-6-yl)-.alpha.-isopropenylacetate or (1R,5S)-.alpha.-(3-substituted-7-oxo-4-oxa-2,6-diazabicyclo-[3.2.0]hept-2-en-6-yl)-.alpha.-isopropylideneacetate with a primary alcohol in the presence of an acid. The products are useful intermediates for preparing oxadethiacephalosporins.

    摘要翻译： α - [3（R） - 取代的氨基-4（R） - 取代的烷氧基-2-氧代 - 氮杂环丁烷-1-基]-α-异丙烯基乙酸酯（Ia）和α-[3（R） - 取代的氨基-4 （3-甲氧基-4-氧代-2,6-二氧代-4-氧杂-4-氮杂环丁烷-1-基）-α-异亚丙基乙酸酯（Ⅰb）由（1R，5S）-α-（3-取代-7-氧代-4-氧代 - 二氮杂双环[3.2.0]庚-2-烯-6-基）-α-异丙烯基乙酸酯或（1R，5S）-α-（3-取代-7-氧代-4-氧杂-2,6-二氮杂双环[3.2 .0]庚-2-烯-6-基）-α-异亚丙基乙酸酯与伯醇在酸存在下反应。 该产品是制备硫代硫菌醚的有用中间体。

    Alkenylsilylazetidinone intermediates for carbapenems
    10.
    发明授权
    Alkenylsilylazetidinone intermediates for carbapenems 失效
    碳青霉烯类烯基甲硅烷基氮杂环丁酮中间体

    公开(公告)号：US4960880A

    公开(公告)日：1990-10-02

    申请号：US247264

    申请日：1988-09-21

    申请人： Shoichiro Uyeo

    发明人： Shoichiro Uyeo

    IPC分类号： C07D205/08 ,  C07F7/10 ,  C07F7/18

    CPC分类号： C07F7/186 ,  C07D205/08 ,  C07F7/10

    摘要： An intermediate for synthesizing carbapenems is produced through(1) a reaction of 4-(leaving group substituted)-2-azetidinone (I) with (alk-2-enyl)halosilane (II) to afford 4-(leaving group substituted)-1-(alk-2-enyl)silyl-2-azetidinone (III) and then(2) a reaction of the product 4-(leaving group substituted)-1-alk-2-enyl)silyl-2-azetidinone (III) with acid to give the corresponding 4-(alk-2-enyl)-2-azetidinone (IV). ##STR1## (The symbols are defined in the specification)