专利号:US-9518014-B2 优先权日:2012-07-20 标 题:Process for synthesis of ezetimibe and intermediates used in said process 发明人:DING KUILING; WANG XIAOMING; WANG ZHENG 权利人:SHANGHAI INST ORGANIC CHEMISTRY CAS 摘要:A process for the production of ezetimibe and intermediates used in said process are disclosed. A kind of Morita-Baylis-Hillman adduct can be altered to chiral carboxylic acid derivatives of β-arylamino α-methylene with high activity and selectivity by means of ally lamination reaction, and the above carboxylic acid derivatives of β-arylamino α-methylene can be altered to the chiral intermediates of ezetimibe by means of simple conversion and further synthesized into the chiral drug ezetimibe. The synthesis route introduces chirality through the use of a chiral catalysis method, thereby avoiding the use of the chiral auxiliary oxazolidinone; and the route is economical and eco-friendly.
专利号:US-6096883-A 优先权日:1996-05-31 标 题 :3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones 发明人:WU GEORGE G; CHEN XING; WONG YEE-SHING; SCHUMACHER DORIS P; STEINMAN MARTIN 权利人:SCHERING CORP 摘要:The invention relates to intermediates of the formulae ##STR1## said intermediates being useful in a process for producing a compound of the formula ##STR2## wherein Bn is benzyl and R 1 , 2 and R 3 are as defined in the specification,
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:WO-2012173504-A2 优先权日:2011-06-15 标 题 :Method for synthesis of the substituted azetidinones and intermediates for their synthesis
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:CA-2731924-A1 优先权日:2008-07-30 标 题 :Process for the synthesis of ezetimibe and intermediates useful therefor
参考标题:Visible-Light Photocatalytic Synthesis Of Amines From Imines Via Transfer Hydrogenation Using Quantum Dots As Catalysts 作者:Zi-Wei Xi,Lei Yang,Dan-Yan Wang,Chao-Dan Pu,Yong-Miao Shen,Chuan-De Wu,Xiao-Gang Peng |发布日期:2018.10.5 摘要:Core/shell Quantum Dots (Qds) Can Be Used As Stable And Highly Active Photoredox Catalysts For Efficient Transfer Hydrogenation Of Imines To Amines With Thiophenol As A Hydrogen Atom Donor. This Reaction Proceeds Via A Proton-Coupled Electron Transfer (Pcet) From The Qds Conduction Band To The Protonated Imine Followed By Hydrogen Atom Transfer From The Thiophenol To The α-Aminoalkyl Radical. This Precious
合成参考文献
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2004). 摘要:Green, J. R., Science of Synthesis, (2006) 8, 452.