发明名称 |
PROCESSES FOR THE PREPARATION OF (3R,4S)-4-((4-BENZYLOXYL)PHENYL)-1-(4-FLUOROPHENYL)-3-HYDROXYPROPYL)-2-AZETIDINONE, AN INTERMEDIATE FOR THE SYNTHESIS OF EZETIMIBE |
摘要 |
<p>The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a) having an enantiomeric purity of at least about 97.5%. The invention also encompasses Compound 2a having a chemical purity of at least about 97%. The invention further encompasses processes for preparing Compound 2a from Compound 1 having the following formula: The invention also encompasses processes for preparing a compound having the following formula: from a compound having the following formula: wherein R is selected from the group consisting of: H or a hydroxyl protecting group. The invention also encompasses processes for preparing Compound 2a, preferably to form Compound 2a-Form 01. Also included are processes for preparing ezetimibe from Compound 2a-Form 01 or Compound 2a prepared according to the invention, compositions containing such ezetimibe, and methods for reducing cholesterol using such compositions.</p> |
申请公布号 |
IL186326(D0) |
申请公布日期 |
2008.01.20 |
申请号 |
IL20070186326 |
申请日期 |
2007.10.07 |
申请人 |
TEVA PHARMACEUTICAL INDUSTRIES LTD.;PERLMAN, NURIT;KANSAL, VINOD KUMAR;GUPTA, NITIN;TYAGI, BHUPENDRA;AHMAD, SUHAIL |
发明人 |
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分类号 |
C07D |
主分类号 |
C07D |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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