广州化工
廣州化工
엄주화공
GUANGZHOU CHEMICAL INDUSTRY AND TECHNOLOGY
2014年
18期
105-106,118
,共3页
依泽替米贝%选择性胆固醇吸收抑制剂%不对称还原%CBS催化剂
依澤替米貝%選擇性膽固醇吸收抑製劑%不對稱還原%CBS催化劑
의택체미패%선택성담고순흡수억제제%불대칭환원%CBS최화제
Ezetimibe%selective cholesterol absorption inhibitor%asymmetric reduction%CBS catalyst
(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。
(4S)-3-[(5S)-5-(4-氟苯基)-5-羥基戊酰基]-4-苯基-1,3-氧氮雜環戊烷-2-酮(1)是依澤替米貝的重要中間體,依澤替米貝是第一箇選擇性膽固醇吸收抑製劑,它可同時榦擾食物來源的膽固醇及腸肝循環中由肝髒閤成的膽固醇的吸收,而對其它營養成分的吸收併不產生影響。本文利用原位生成的R-OMe-CBS催化劑不對稱還原得到1,反應條件溫和、成本降低,同時實更加適應實際的工業生產。
(4S)-3-[(5S)-5-(4-불분기)-5-간기무선기]-4-분기-1,3-양담잡배무완-2-동(1)시의택체미패적중요중간체,의택체미패시제일개선택성담고순흡수억제제,타가동시간우식물래원적담고순급장간순배중유간장합성적담고순적흡수,이대기타영양성분적흡수병불산생영향。본문이용원위생성적R-OMe-CBS최화제불대칭환원득도1,반응조건온화、성본강저,동시실경가괄응실제적공업생산。
(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.