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1. 发明授权

EP0224059B1 Azetidinone derivative and process for preparing the same 失效
标题翻译： AZETIDINONE衍生物及其制备方法
公开(公告)号：EP0224059B1
公开(公告)日：1992-04-15
申请号：EP86114952.4
申请日：1986-10-28
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07D205/08 , C07B53/00
CPC分类号： C07F7/186 , C07D205/08 , Y02P20/55

2. 发明公开

EP0224059A1 Azetidinone derivative and process for preparing the same 失效
标题翻译：其生产的氮杂环丁酮衍生物和方法。
公开(公告)号：EP0224059A1
公开(公告)日：1987-06-03
申请号：EP86114952.4
申请日：1986-10-28
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07D205/08 , C07B53/00
CPC分类号： C07F7/186 , C07D205/08 , Y02P20/55
摘要： An azetidinone derivative having the general formula (I):
wherein R¹ and R² are hydrogen atom or a protective group and R³ is an alkyl group or hydrogen atom, a process for preparing the same, and a process for preparing an azetidinone derivative having the general formula (II):
wherein R¹, R² and R³ are as above. The azetidinone derivative (I) of the present invention can be converted into an important intermediate of lβ-methylcarbapenem antibiotics by a selective reduction of the double bond.

3. 发明公开

EP0209886A2 beta-N-substituted aminothiol ester and process for preparing the same 失效
标题翻译： β-N-取代基氨基硫醇和Verfahren zur deren Herstellung。
公开(公告)号：EP0209886A2
公开(公告)日：1987-01-28
申请号：EP86110029.5
申请日：1986-07-22
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07F7/08 , C07D205/08
CPC分类号： C07F7/0818 , C07D205/08
摘要： β-N-Substituted aminothiol ester represented by the general formula (I) :
wherein R' is an alkyl group or an aryl group and R 2 is an aralkyl group, a process for preparing the same, and an azetidinone derivative represented by the general formula (VI) :
wherein R 2 is as above.
The β-N-subsituted aminothiol ester (I) of the present invention can be an excellent intermediate for preparing the β-lactam (II).
摘要翻译：由通式（I）表示的β-取代的氨基硫醇酯：... 其中R 1是烷基或芳基，R 2是芳烷基，其制备方法，和由通式（VI）表示的氮杂环丁酮衍生物：... 其中R 2如上。本发明的β-N-取代的氨基硫醇酯（I）可以是制备β-内酰胺（II）的优良中间体。

4. 发明授权

EP0181581B1 beta-Aminothiol ester and process for preparing thereof 有权
标题翻译： BETA-AMINOTHIOL ESTER及其制备方法
公开(公告)号：EP0181581B1
公开(公告)日：1988-07-13
申请号：EP85113926.1
申请日：1985-11-01
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07C153/09
CPC分类号： C07D205/08 , C07C327/00 , Y02P20/55

5. 发明公开

EP0209886A3 beta-N-substituted aminothiol ester and process for preparing the same 失效
标题翻译： BETA-N-取代的氨基酸酯及其制备方法
公开(公告)号：EP0209886A3
公开(公告)日：1987-05-13
申请号：EP86110029
申请日：1986-07-22
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07F07/08 , C07D205/08
CPC分类号： C07F7/0818 , C07D205/08
摘要： β-N-Substituted aminothiol ester represented by the general formula (I) :
wherein R' is an alkyl group or an aryl group and R 2 is an aralkyl group, a process for preparing the same, and an azetidinone derivative represented by the general formula (VI) :
wherein R 2 is as above. The β-N-subsituted aminothiol ester (I) of the present invention can be an excellent intermediate for preparing the β-lactam (II).

6. 发明授权

EP0209886B1 beta-N-substituted aminothiol ester and process for preparing the same 失效
标题翻译： BETA-N-取代的氨基酸酯及其制备方法
公开(公告)号：EP0209886B1
公开(公告)日：1990-03-21
申请号：EP86110029.5
申请日：1986-07-22
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07F7/08 , C07D205/08
CPC分类号： C07F7/0818 , C07D205/08

7. 发明公开

EP0181581A1 beta-Aminothiol ester and process for preparing thereof 有权
标题翻译： Beta-Aminothiolester和Verfahren zu ihrer Herstellung。
公开(公告)号：EP0181581A1
公开(公告)日：1986-05-21
申请号：EP85113926.1
申请日：1985-11-01
申请人： SAGAMI CHEMICAL RESEARCH CENTER
发明人： Shibasaki, Masakatsu , Iimori, Takamasa
IPC分类号： C07C153/09
CPC分类号： C07D205/08 , C07C327/00 , Y02P20/55
摘要： β-Aminothiol ester having the general formula (l):

wherein R 1 is alkyl group or aryl group and R 2 and R 3 are protective groups. β-Aminothiol ester of the present invention having the general formula (I) is prepared by reacting β-hydroxythiol ester having the general formula (lll):

wherein R' is as above, with boron compound having the general formula (lV):

wherein R and R' are alkyl group or cycloalkyl group or, taken together, they can form a ring including boron atom in the presence of tertiary amine, the obtained reaction mixture being reacted with imine having the general formula (V):

wherien R 2 and R 3 are protective groups, followed by treating the resultant with hydrogen peroxide.
摘要翻译：具有通式（I）的β-氨基硫醇酯：... 其中R 1为烷基或芳基，R 2和R 3为保护基。具有通式（I）的本发明的β-氨基硫醇酯通过使具有通式（III）的β-羟基硫醇酯：其中R 1如上所述与具有通式（IV）：... 其中R和R min是烷基或环烷基，或者它们可以一起在叔胺存在下形成包含硼原子的环，所得反应混合物与亚胺反应具有通式（Ⅴ）：... ...乳清R 2和R 3是保护基，然后用过氧化氢处理所得物。

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