-
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。 -
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。 -
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。 -
公开(公告)号:US4504659A
公开(公告)日:1985-03-12
申请号:US543939
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.
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。
-
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。
-
6.
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。 -
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) )。
-
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。
-
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.
-
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。
-
-
-
-
-
-
-
-
-