首页> 外国专利> 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

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

机译:(3R,4S)-4-((4-苄氧基)苯基)-1-(4-氟苯基)-3-羟丙基)-2-氮杂环丁酮的制备方法

摘要

The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-l-(4-fluorophenyl)-3- (3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a). The invention further encompasses processes tor preparing Compound 2a from Compound 1. The invention also encompasses processes for preparing a compound having Formula (A) from a compound having the formula (B); 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.
机译:本发明包括(3R,4S)-4-((4-苄氧基)苯基)-1-(4-氟苯基)-3-(3-(4-氟苯基)-3-氧丙基)-2-氮杂环丁酮(化合物2a )。本发明进一步包括由化合物1制备化合物2a的方法。本发明还涵盖由具有式(B)的化合物制备具有式(A)的化合物的方法;其中R选自由以下组成的组:H或羟基保护基。本发明还包括制备化合物2a的方法,优选形成化合物2a-形式01。还包括由根据本发明制备的化合物2a-形式01或化合物2a制备依泽替米贝的方法,包含此类依泽替米贝的组合物和还原方法使用这种组合物的胆固醇。

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