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-2010216998-A1 优先权日:2007-09-18 标题:Facile 'One Pot' Process for Apomorphine From Codeine 发明人:GURUSAMY NARAYANASAMY 权利人:MALLINCKRODT INC 摘要:An improved method for producing apomorphine and derivatives thereof is provided. The method is a convenient ‘one-pot’ process, comprising the conversion of codeine into apomorphine without isolating the apocodeine intermediate. Use of water reactive scavengers, reagents that will react irreversibly with water, decreases side product formation and allows the use of milder reaction conditions. This one-pot synthesis of apomorphine from codeine provides a faster reaction with improved yields at temperatures lower as compared to conventional methods. The lower operating temperatures and less volatile reactants make the method particularly useful for large-scale manufacturing.
专利号:US-5118836-A 优先权日:1989-11-08 标题:Optically active fluorine-containing 3-hydroxybutyric acid esters and process for producing the same 发明人:TANIDA KAICHI; SUZUKI YOSHIICHI 权利人:SHOWA SHELL SEKIYU 摘要:An optically active (3R)- or (3S)-fluorine-containing-3-hydroxybutyric acid ester represented by the formula: ##STR1## wherein R represents an alkyl group of C 3 -C 16 and A represents CF 3 , CHF 2 or CH 2 F, which is useful for synthesis of optically active substances, is prepared with high optical purity by ester exchange reaction between an alcohol represented by the formula: n n ROH n n wherein R is as defined above and optically active (3R)- or (3S)-fluorine-containing-3-hydroxybutyric acid ethyl ester of ##STR2## in the presence of an ammonium salt of sulfonic acid.
专利号:US-11667660-B2 优先权日:2018-11-22 标题 :Pyridinium salts as activators in the synthesis of stereodefined oligonucleotides 发明人:HANSEN DENNIS JUL; FUNDER ERIK DAA 权利人:ROCHE INNOVATION CT COPENHAGEN AS 摘要:The present invention relates to a method for preparing stereodefined phosphorothioate oligonucleotides, especially locked stereodefined phosphorothioate oligonucleotides with a high yield, using pyridinium acidic salts as a coupling activator.
专利号:EP-2004639-A2 优先权日:2006-04-10 标 题:Processes for the synthesis of azetidinone
专利号:EP-3883941-A1 优先权日:2018-11-22 标 题:Pyridinium salts as activators in the synthesis of stereodefined oligonucleotides
参考文献:10.1007/s11164-021-04592-7 摘要:Sadeghpour M, Olyaei A. Recent advances in the synthesis of bis(pyrazolyl)methanes and their applications. Research on Chemical Intermediates. 2021 Oct 08;47(11):4399–441. doi: 10.1007/s11164-021-04592-7. 参考文献:10.1007/s11164-010-0222-6 摘要:Wang R, Sun M, Jiang H. Solvent-free tetrahydropyranylation of alcohols catalyzed by amine methanesulfonates. Research on Chemical Intermediates. 2010 Nov 24;37(1):61–7. doi: 10.1007/s11164-010-0222-6.