发明名称 |
Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe |
摘要 |
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
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申请公布号 |
US2010010212(A1) |
申请公布日期 |
2010.01.14 |
申请号 |
US20090583305 |
申请日期 |
2009.08.17 |
申请人 |
KANSAL VINOD KUMAR;AHMAD SUHAIL;TYAGI BHUPENDRA;GUPTA NITIN |
发明人 |
KANSAL VINOD KUMAR;AHMAD SUHAIL;TYAGI BHUPENDRA;GUPTA NITIN |
分类号 |
C07D205/08;A61K31/397 |
主分类号 |
C07D205/08 |
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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