专利号:US-9938282-B2 优先权日:2014-02-05 标 题:Expedient synthesis of sitagliptin 发明人:JANAGANI SATYANARAYANA; THADURI VENKATESHWAR KUMAR; VAMARAJU RAVISANKAR 权利人:STEREOKEM INC 摘要:Novel intermediates are disclosed as intermediates for preparation of a Sitagliptin. A novel synthetic method to prepare Sitagliptin using the said intermediates is also disclosed.
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.
专利号:US-2018222936-A1 优先权日:2011-07-19 标 题:Methods for the synthesis of functionalized nucleic acids
专利号:EP-3102580-A2 优先权日:2014-02-05 标题 :Expedient synthesis of sitagliptin
专利号:CA-2842358-A1 优先权日:2011-07-19 标题 :Methods for the synthesis of functionalized nucleic acids
专利号:JP-6128529-B2 优先权日:2011-07-19 标题:Methods for the synthesis of functionalized nucleic acids
参考标题:The Ring Opening Of 3,4-Dichloro-1,2,5-Thiadiazole With Metal Amides. A New Synthesis Of 3,4-Disubstituted-1,2,5-Thiadiazoles 作者:Alain Merschaert,Pascal Boquel,Hugo Gorissen,Jean-Pierre Van Hoeck,Alfio Borghese,Luc Antoine,Vincent Mancuso,Anne Mockel,Michel Vanmarsenille |发布日期:2006.11 摘要:We Have Developed A New Synthesis Of 3,4-Disubstituted-1,2,5-Thiadiazoles. The Methodology Is Based On The Ring Opening Of Readily Available 3,4-Dichloro-1,2,5-Thiadiazole With Metal Amides To Afford A Stable Synthon, Which Is Then Transformed Into The 3,4-Disubstituted-1,2,5-Thiadiazole Derivatives Via Two Consecutive Reactions With O-, S-, N- Or C-Nucleophiles.
合成参考文献
参考文献:10.1007/s00216-015-9068-5 摘要:Hammann S, Englert M, Müller M, Vetter W. Accelerated separation of GC-amenable lipid classes in plant oils by countercurrent chromatography in the co-current mode. Analytical and Bioanalytical Chemistry. 2015 Oct 05;407(30):9019–28. doi: 10.1007/s00216-015-9068-5.