公开(公告)号：EP0048136A2

公开(公告)日：1982-03-24

申请号：EP81304154.8

申请日：1981-09-10

申请人： SYNTEX PHARMACEUTICALS INTERNATIONAL LIMITED

发明人： Tsuchihashi, Genichi ,  Mitamura, Shuichi ,  Kitajima, Kouji

IPC分类号： C07C67/333 ,  C07C143/68

CPC分类号： C07D333/24 ,  C07C43/307 ,  C07C43/315 ,  C07C45/46 ,  C07C45/63 ,  C07C49/80 ,  C07C51/00 ,  C07C57/30 ,  C07C59/64 ,  C07C309/00 ,  C07D209/46 ,  C07D303/48 ,  C07D317/20 ,  C07D317/24 ,  C07D333/22 ,  C07C49/84 ,  C07C57/32 ,  C07C63/06

摘要： A process for preparing an alpha-aromatic group substituted alkanoic acid or its ester of the general formula
wherein Ar represents an aromatic group and R' represents a hydrogen atom or a saturated aliphatic group, or Ar and R 1 may form a condensed ring together with the carbon atom to which they are bonded; and R 2 represents a hydrogen atom, an alkyl group, or a hydroxyalkyl group. characterized in that an alpha-sulfonyloxyketone acetal of the general formula
wherein R 3 and R 4 , independently from each other, represent an alkyl group, or taken together, represent an alkylene group; R 5 represents a substituted or unsubstituted alkyl group or an aromatic group; and Ar and R 1 are as defined above, is hydrolyzed, or treated with an agent having affinity for oxygen: and novel intermediate compounds of the general formula (II) used in aforesaid process.

摘要翻译： 一种用于制备α-芳基substituiertem链烷酸或它的通式酯过程 worin的Ar darstellt芳族基团和R <1> darstellt一个氢原子或饱和脂肪族基团，或Ar及R <1> 可以与它们所结合的碳原子一起形成稠合环; 且R <2> darstellt的氢原子的烷基，或羟烷基，在上述通式 worin的R那样的α-磺酰氧基缩醛为特征的<3>和R <4>，从海誓山盟unabhängig， 表示到烷基。 或者一起，在亚烷基代表; [R <6> darstellt一个substituiertem奥德unsubstituiertem烷基或芳族基团; 且Ar和R <1>如上文所定义，被hydrolyred，或与具有对氧的亲和性的试剂处理; 并且在上述方法中使用的通式（II）的新的中间体化合物。

公开(公告)号：EP0151702B1

公开(公告)日：1987-11-25

申请号：EP84113585.8

申请日：1981-09-10

申请人： SYNTEX PHARMACEUTICALS INTERNATIONAL LIMITED

发明人： Tsuchihashi, Genichi ,  Mitamura, Shuichi ,  Kitajima, Kouji

IPC分类号： C07C43/315 ,  C07D209/46 ,  C07D333/22

CPC分类号： C07D333/24 ,  C07C43/307 ,  C07C43/315 ,  C07C45/46 ,  C07C45/63 ,  C07C49/80 ,  C07C51/00 ,  C07C57/30 ,  C07C59/64 ,  C07C309/00 ,  C07D209/46 ,  C07D303/48 ,  C07D317/20 ,  C07D317/24 ,  C07D333/22 ,  C07C49/84 ,  C07C57/32 ,  C07C63/06

公开(公告)号：EP0151702A2

公开(公告)日：1985-08-21

申请号：EP84113585.8

申请日：1981-09-10

申请人： SYNTEX PHARMACEUTICALS INTERNATIONAL LIMITED

发明人： Tsuchihashi, Genichi ,  Mitamura, Shuichi ,  Kitajima, Kouji

IPC分类号： C07C43/315 ,  C07D209/46 ,  C07D333/22

CPC分类号： C07D333/24 ,  C07C43/307 ,  C07C43/315 ,  C07C45/46 ,  C07C45/63 ,  C07C49/80 ,  C07C51/00 ,  C07C57/30 ,  C07C59/64 ,  C07C309/00 ,  C07D209/46 ,  C07D303/48 ,  C07D317/20 ,  C07D317/24 ,  C07D333/22 ,  C07C49/84 ,  C07C57/32 ,  C07C63/06

摘要： Alpha-hydroxyketone acetals of the formula:
wherein Ar represents an aromatic group, R 1 represents a hydrogen atom or a saturated aliphatic group, or Ar and R' form a condensed ring together with the carbon atom to which they are bonded, and R 3 and R 4 independently represent alkyl groups or together represent an alkylene group, subject to the proviso that Ar does not represent phenyl or 4-chlorophenyl when R' is a hydrogen atom. The acetals (VI) can be converted into alpha-sulfonyloxyketone acetals and thence into alpha-aromatic group substituted alkanoic acids or esters.

摘要翻译： 下式的α-羟基酮缩醛：其中Ar表示芳族基团，R 1表示氢原子或饱和脂肪族基团，或Ar和R 1与碳原子一起形成稠环， 它们是键合的，R 3和R 4独立地表示烷基或一起表示亚烷基，条件是当R 1是氢原子时Ar不代表苯基或4-氯苯基。 缩醛（VI）可以转化成α-磺酰氧基酮缩醛，然后转化成α-芳族取代的链烷酸或酯。

公开(公告)号：EP0048136B1

公开(公告)日：1986-06-11

申请号：EP81304154.8

申请日：1981-09-10

申请人： SYNTEX PHARMACEUTICALS INTERNATIONAL LIMITED

发明人： Tsuchihashi, Genichi ,  Mitamura, Shuichi ,  Kitajima, Kouji

IPC分类号： C07C67/333 ,  C07C143/68

CPC分类号： C07D333/24 ,  C07C43/307 ,  C07C43/315 ,  C07C45/46 ,  C07C45/63 ,  C07C49/80 ,  C07C51/00 ,  C07C57/30 ,  C07C59/64 ,  C07C309/00 ,  C07D209/46 ,  C07D303/48 ,  C07D317/20 ,  C07D317/24 ,  C07D333/22 ,  C07C49/84 ,  C07C57/32 ,  C07C63/06

公开(公告)号：EP0151702A3

公开(公告)日：1985-10-02

申请号：EP84113585

申请日：1981-09-10

申请人： SYNTEX PHARMACEUTICALS INTERNATIONAL LIMITED

发明人： Tsuchihashi, Genichi ,  Mitamura, Shuichi ,  Kitajima, Kouji

IPC分类号： C07C43/315 ,  C07D209/46 ,  C07D333/22

CPC分类号： C07D333/24 ,  C07C43/307 ,  C07C43/315 ,  C07C45/46 ,  C07C45/63 ,  C07C49/80 ,  C07C51/00 ,  C07C57/30 ,  C07C59/64 ,  C07C309/00 ,  C07D209/46 ,  C07D303/48 ,  C07D317/20 ,  C07D317/24 ,  C07D333/22 ,  C07C49/84 ,  C07C57/32 ,  C07C63/06

摘要： Alpha-hydroxyketone acetals of the formula:
wherein Ar represents an aromatic group, R 1 represents a hydrogen atom or a saturated aliphatic group, or Ar and R' form a condensed ring together with the carbon atom to which they are bonded, and R 3 and R 4 independently represent alkyl groups or together represent an alkylene group, subject to the proviso that Ar does not represent phenyl or 4-chlorophenyl when R' is a hydrogen atom. The acetals (VI) can be converted into alpha-sulfonyloxyketone acetals and thence into alpha-aromatic group substituted alkanoic acids or esters.

公开(公告)号：EP0091757A1

公开(公告)日：1983-10-19

申请号：EP83301808.8

申请日：1983-03-30

申请人： SYNTEX PHARMACEUTICALS INTERNATIONAL LIMITED

发明人： Tsuchihashi, Genichi ,  Mitamura, Shuichi ,  Kitajima, Koji ,  Kobayashi, Kumi

IPC分类号： C07C125/065 ,  C07C93/14

CPC分类号： C07C51/09 ,  C07C59/64

摘要： A manufacturing method is described for the preparation of optically active 1-(6-methoxy-2-naphthyl)-2-(alkoxycarbonyl)amino-1-propanone
its derivatives and their halo analogs. These compounds are useful intermediates in the preparation of 2-(6-methoxy-2-naphthyl)propionic acid, which is useful pharmaceutically, e.g. as an anti-inflammatory, analgesic and anti-pyretic agent.