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-5512701-A 优先权日:1995-06-07 标题:Process for the synthesis of vinyl sulfenic acid derivatives 发明人:HOARD DAVID W; LUKE WAYNE D 权利人:LILLY CO ELI 摘要:The present invention is directed to a new process for the synthesis of vinyl sulfenic acid derivatives. These compounds are useful for the synthesis of benzo[b]thiophenes, in particular 2-aryl-benzo[b]thiophenes.
专利号:US-2023287032-A1 优先权日:2020-08-14 标 题:Synthesis of fluorinated nucleotides 发明人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO 权利人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO; MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (O—{[(2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-3-hydroxyoxolan-2-yl]methyl}O,O-dihydrogen phosphorothioate, also known as 2′-(S)-fluoro-thio-adenosine monophosphate or 2′-F-thio-AMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
专利号:US-5606075-A 优先权日:1995-06-07 标 题:Process for the synthesis of benzo[b]thiophenes 发明人:HOARD DAVID W; LUKE WAYNE D 权利人:LILLY CO ELI 摘要:The present invention is directed to new processes for the synthesis of 2-aryl benzo[b]thiophenes.
专利号:EP-2030975-A1 优先权日:2007-08-06 标 题:CEFDINIR synthesis process 发明人:MANCA ANTONIO; FILIPPI MAURO; SALA BRUNO MAURIZIO; MONGUZZI RICCARDO AMBROGIO; FOGLIATO GIOVANNI 权利人:ACS DOBFAR SPA 摘要:Cefdinir preparation by synthesis of new key intermediates, isolable as variously solvated species complexed with thiophosphoric acid derivatives or with phosphoric acid derivatives.
专利号:US-9605019-B2 优先权日:2011-07-19 标 题:Methods for the synthesis of functionalized nucleic acids 发明人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL 权利人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL; WAVE LIFE SCIENCES LTD 摘要:The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.