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1. 发明授权

US4220766A Oxazolines 失效
标题翻译：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。

2. 发明授权

US4366316A 1-Oxadethiacepham compounds and process for producing said compounds 失效
标题翻译： 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。

3. 发明授权

US4271296A Oxazolines 失效
公开(公告)号：US4271296A
公开(公告)日：1981-06-02
申请号：US112145
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.

4. 发明授权

US4271295A Oxazolines 失效
标题翻译：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。

5. 发明授权

US4183855A Oxazolinoazetidinylbutyric acid derivatives 失效
标题翻译：恶唑嗪并吖丁啶丁酸衍生物
公开(公告)号：US4183855A
公开(公告)日：1980-01-15
申请号：US881054
申请日：1978-02-24
申请人： Mitsuru Yoshioka , Shoichiro Uyeo , Teruji Tsuji , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
发明人： Mitsuru Yoshioka , Shoichiro Uyeo , Teruji Tsuji , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
IPC分类号： C07D507/00 , C07D205/085 , C07D498/04 , C07D505/00
CPC分类号： C07D205/085 , C07D505/00
摘要： Intermediates (I) for preparing a potent antibacterial, 1-oxadethiacephalosporin, are shown by the following formula ##STR1## (wherein R is a group of acyl-minus-carbonyl derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group;Y is a nucleophilic group; andZ is a leaving group)and prepared from the corresponding exomethylene compound (II) by addition of a compound of formula: Y-Z (in which Y and Z are as defined above).
摘要翻译：通过下式表示制备有效抗菌性1-羟基乙醚孢子的中间体（I）（其中R是衍生自羧酸或碳酸的酰基 - 负 - 羰基基团; COB是羧基或被保护的羧基; X是氢或亲核基团; Y是亲核基团; Z是离去基团），并且由相应的外亚甲基化合物（II）通过加入式YZ化合物（其中Y和Z定义如上））。

6. 发明授权

US4478997A 1-Oxadethiacepham compounds 失效
标题翻译： 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。

7. 发明授权

US4233216A Azetidinone derivatives and production thereof 失效
标题翻译：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。

8. 发明授权

US4443598A 1-Oxadethiacepham compounds 失效
标题翻译： 1-氧杂十八胺化合物
公开(公告)号：US4443598A
公开(公告)日：1984-04-17
申请号：US374862
申请日：1982-05-04
申请人： Mitsuru Yoshioka , Uyeo Shoichiro , Yoshio Hamashima , Ikuo Kikkawa , Teruji Tsuji , Wataru Nagata
发明人： Mitsuru Yoshioka , Uyeo Shoichiro , 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 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. 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 + TR 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。

9. 发明授权

US4604460A 1-oxadethiacepham compounds 失效
标题翻译： 1-恶嗪硫醚化合物
公开(公告)号：US4604460A
公开(公告)日：1986-08-05
申请号：US542520
申请日：1983-10-17
申请人： Mitsuru Yoshioka , Uyeo Shoichiro , Yoshio Hamashima , Ikuo Kikkawa , Teruji Tsuji , Wataru Nagata
发明人： Mitsuru Yoshioka , Uyeo Shoichiro , 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 preparaing 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 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 aboveby 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-氧环孢菌素的中间体：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 + TR 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。

10. 发明授权

US4533730A 1-Oxadethiacepham compounds 失效
标题翻译： 1-氧杂十八胺化合物
公开(公告)号：US4533730A
公开(公告)日：1985-08-06
申请号：US543940
申请日：1983-10-19
申请人： Mitsuru Yoshioka , Uyeo Shoichiro , Yoshio Hamashima , Ikuo Kikkawa , Teruji Tsuji , Wataru Nagata
发明人： Mitsuru Yoshioka , Uyeo Shoichiro , 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-oxacephalosporins 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. 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为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 + TR 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。

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