US2005197501A1PendingUtilityA1

Processes for preparing calcium salt forms of statins

Assignee: TEVA PHARMAPriority: Nov 16, 2000Filed: May 2, 2005Published: Sep 8, 2005
Est. expiryNov 16, 2020(expired)· nominal 20-yr term from priority
C07D 209/24C07D 309/30Y02P20/55C07D 207/34C07D 215/14C07D 213/55C07D 239/42C07D 405/06C07F 3/04
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Claims

Abstract

Processes for preparing a calcium salt of a statin from an ester derivative or protected ester derivative of the statin by using calcium hydroxide are provided. The ester or protected ester derivative is contacted with calcium hydroxide to obtain the calcium salt. Preferred statins are rosuvastatin, pitavastatin and atorvastatin, simvastatin and lovastatin. In processes beginning with a protected statin ester derivative, the protecting group is hydrolyzed during salt formation by contact with calcium hydroxide, or is contacted with an acid catalyst followed by contact with calcium hydroxide.

Claims

exact text as granted — not AI-modified
1 . A process for preparing a calcium salt of a statin having the formula:  
       
         
           
           
               
               
           
         
       
       wherein R represents and organic radical, comprising contacting an ester derivative of the statin selected from the group consisting of:  
       
         
           
           
               
               
           
         
       
       with a sufficient amount of calcium hydroxide, wherein R 1  is a C 1  to a C 8  alkyl group, and R 2 , R 3  and R 4  each independently represent hydrogen, or the same or different hydrolyzable protecting group, or R 2  and R 3 , together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group.  
     
     
         2 - 42 . (canceled)

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