CAS: 190595-65-4; (3R,4S)-4-(4-(Benzyloxy)Phenyl)-1-(4-Fluorophenyl)-3-(3-(4-Fluorophenyl)-3-Oxopropyl)Azetidin-2-One

上下游产品

CAS号1206694-77-0 (3R,4S)-4-[4-(b... | CAS号352-13-6 4-氟苯基溴化镁 | CAS号181705-93-1 4-氟苯溴化锌 | CAS号231301-01-2 (3R,4S)-4-(4-(b... | CAS号1380431-24-2 (3R,4S)-4-(4-(b... | CAS号133472-27-2 chlorozinc(1+),... | CAS号163222-32-0 4'-O-苄氧依折麦布 | CAS号163380-15-2 (3R,4S,3'R)-1-(... | CAS号163222-33-1 依泽替米贝 | CAS号163380-16-3 依折麦布(3R)-异构体 | CAS号163380-20-9 依折麦布二乙酸酯 | CAS号191330-56-0 依折麦布酮

3-{(2R,3S)-3-[(4-Fluorophenyl)Amino]-2-[2-(4-Fluorophenyl)-5,5-Dimethyl-1,3-Dioxan-2-Yl]-3-[4-(Benzyloxy)Phenyi]Propanoyl}-(4S)-4-Phenyl-1,3-Oxazolidin-2-One置于甲酸,N,O-Bis(Trimethylsilyl)Acetamide,四丁基氟化铵体系中,用 二氯甲烷,甲苯 用作溶剂,化学反应 60.0H,反应生成(3R,4S)-4-[4-(苄氧基)苯基]-1-(4-氟苯基)-3-[3-(4-氟苯基)-3-氧代丙基]氮杂环丁烷-2-酮
参考文献:依替米贝的中间体及其合成方法与依替米贝的合成方法
标题:依替米贝的中间体及其合成方法与依替米贝的合成方法
摘要:本发明提供了依替米贝的中间体及其合成方法与依替米贝的合成方法,该方法合成路线短.本发明以氟苯为起始原料,氟苯依次与戊二酸酐,4(S)‑4‑苯基恶唑烷酮发生酰化反应生成ii后,再用2,2‑二取代‑1,3‑丙二醇对羰基进行保护得到化合物iii,然后化合物iii与化合物iv在四氯化钛催化下生成化合物v,化合物v环合生成化合物vi,化合物vi水解得到化合物vii,化合物vii经硼烷类手性还原剂还原以及氢化脱除苄基保护基得到依替米贝.该方法收率高,副反应少,适合于工业化大生产.

专利信息

专利号:US-2008032964-A1
优先权日:2006-04-10
标题:Process for the synthesis of azetidinone
发明人：KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.

专利号:US-2010010212-A1
优先权日:2005-09-08
标题 :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
发明人：KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN
权利人:KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN
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: n n n n n n n n n n The invention also encompasses processes for preparing a compound having the following formula: n n n n n n n n n n from a compound having the following formula: n n n n n n n n n n 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

专利号:US-9040688-B2
优先权日:2009-03-31
标 题 :Intermediates in the preparation of 1,4-diphenyl azetidinone
发明人：SRIVASTAVA DHANANJAI; SHAKYA RAJIV KUMAR; CHAUDHARI NAMRATA ANIL; ANSARI INAMUS SAQLAIN; SINGH GIRIJ PAL
权利人:SRIVASTAVA DHANANJAI; SHAKYA RAJIV KUMAR; CHAUDHARI NAMRATA ANIL; ANSARI INAMUS SAQLAIN; SINGH GIRIJ PAL; LUPIN LTD
摘要:The process of the present invention relates to a method for the synthesis of a 1,4-diphenylazetidinone of formula (VIII) by using novel oxime intermediates.

专利号:US-2010168414-A1
优先权日:2006-03-29
标题 :Processes for preparing ezetimibe and intermediate compounds useful for the preparation thereof
发明人：ESCUDE ANA GAVALDA; BOSCH I LLADO JORDI; NETTEKOVEN ULRIKE
权利人:MEDICHEM SA
摘要:The invention relates, in general, to an improved process for converting compounds of Formula II (below) to compounds of Formula III (below), which are key intermediates for the synthesis of ezetimibe, or to ezetimibe itself, wherein in Formulas II and III, R represents hydrogen, alkyl, or a hydroxyl protecting group (e.g., benzyl group, a substituted benzyl group, or a silyl group). The invention further includes the use of the described process and the use of compounds of Formula III made by the described process for the preparation of ezetimibe.

专利号:US-2007259845-A1
优先权日:2005-09-08
标 题 :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

专利号:EP-1953140-A1
优先权日:2007-01-24
标 题 :Process for the preparation of ezetimibe and derivatives thereof
发明人：STIMAC ANTON; MOHAR BARBARA; STEPHAN MICHEL; BEVC MOJCA; ZUPET ROK; GARTNER ANDREJ; KROSELJ VESNA; SMRKOLJ MATEJ
权利人:KRKA
摘要:The present invention relates to the method of preparing of ezetimibe and in particular to novel intermediates for its synthesis and an improved process for preparing such intermediates. Said intermediates may be obtained in high yields and purity in a fast and cost efficient manner. The present invention relates to a novel crystalline form of ezetimibe as well.