依泽替米贝中间体的新工艺

(4S)-3-[(5S)-5-(4-氟苯基)-5-羟基戊酰基]-4-苯基-1,3-氧氮杂环戊烷-2-酮(1)是依泽替米贝的重要中间体,依泽替米贝是第一个选择性胆固醇吸收抑制剂,它可同时干扰食物来源的胆固醇及肠肝循环中由肝脏合成的胆固醇的吸收,而对其它营养成分的吸收并不产生影响。本文利用原位生成的R-OMe-CBS催化剂不对称还原得到1,反应条件温和、成本降低,同时实更加适应实际的工业生产。

The New Process of Ezetimibe Intermediate

（4S）-3-[（5S）-5-（4-Fluorophenyl ）-5-hydroxypentanoyl ]-4-phenyl-1,3-oxazolidin -2-one（1）, a key intermediate of Ezetimibe, was the first selective cholesterol absorption inhibitor , which can also interfered with the absorption of food sources of cholesterol and enterohepatic circulation of cholesterol synthesis by the liver , and without impact on the absorption of other nutrients .1 was obtained by R-OMe-CBS which was generated in situ .The process was low cost and conditions were mild .It was easy to do commercially production.