公开(公告)号：US08124790B2

公开(公告)日：2012-02-28

申请号：US12734500

申请日：2008-04-04

申请人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoi Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

发明人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoi Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

IPC分类号： C07D207/333 ,  C07D405/06 ,  C07D319/06

CPC分类号： C07D319/06 ,  C07D207/34 ,  C07D405/06

摘要： The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.

摘要翻译： 本发明涉及可用于合成阿托伐他汀的制备方法，更具体地说，一种制备阿托伐他汀的方法在治疗高脂血症方面是有效的，包括保护原料顺式叔丁基-6-取代的C3和C5位的二羟基 -3,5-二羟基己酸酯与原甲酸三烷基酯反应，将末端硝基或氰基还原成胺基，通过与4-氟苯-2-卤代乙酸乙酯和异丁酰氯依次反应进行N-烷基化，用JV，3-二苯基丙酰胺 ，进行脱保护和水解。

公开(公告)号：US20110112309A1

公开(公告)日：2011-05-12

申请号：US12734500

申请日：2008-04-04

申请人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoe Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

发明人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoe Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

IPC分类号： C07D405/06 ,  C07D207/34 ,  C07D319/06

CPC分类号： C07D319/06 ,  C07D207/34 ,  C07D405/06

摘要： The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.

摘要翻译： 本发明涉及可用于合成阿托伐他汀的制备方法，更具体地说，一种制备阿托伐他汀的方法在治疗高脂血症方面是有效的，包括保护原料顺式叔丁基-6-取代的C3和C5位的二羟基 -3,5-二羟基己酸酯与原甲酸三烷基酯反应，将末端硝基或氰基还原成胺基，通过与4-氟苯-2-卤代乙酸乙酯和异丁酰氯依次反应进行N-烷基化，用JV，3-二苯基丙酰胺 ，进行脱保护和水解。