专利号:US-6407223-B1 优先权日:1997-04-25 标 题 :Process for the synthesis of modified P-chiral nucleotide analogues 发明人:STEC WOJCIECH J; WOZNIAK LUCYNA A; CHWOROS ARKADIUSZ; PYZOWSKI JAROSLAW 权利人:POLSKA AKADEMIA NAUK CENIRUM B 摘要:The process of the instant invention is drawn to the synthesis of modified P-chiral nucleotide analogues in the form of pure diastereomers possessing preselected configuration at the P-atom. Oligonucleotides prepared by the method of the invention containing P-chiral compounds have enhanced hybridization and transporting properties.
专利号:WO-2018154244-A1 优先权日:2017-02-24 标题 :Method for the synthesis of pheromones 发明人:QUEVAL PIERRE; CAIJO FRÉDÉRIC; ROUEN MATHIEU; TRIPOTEAU FABIEN 权利人:DEMETA 摘要:The invention relates to a method for the synthesis of pheromones functionalised on one of the ends thereof and comprising at least two conjugated double bonds with a majority stereochemical configuration (E, Z). The reaction is carried out in two steps, comprising: (a) a metathesis reaction between a functionalised olefin and an unsaturated aldehyde, in the presence of at least one specific catalyst selected from the ruthenium complexes comprising a 1,3-diaryl-imidazolidin-2-yl ligand and a styrenyl ether ligand, and (b) the reaction of the product obtained in this way with a triphenylalkylphosphonium salt.
专利号:EP-2589587-A1 优先权日:2011-11-04 标题:Synthesis of nitrogen substituted cyclopropanes 发明人:RASPARINI MARCELLO; TADDEI MAURIZIO; CINI ELENA; MINELLI COSIMA; TURNER NICHOLAS; HUGENTOBLER KATHARINA GLORIA 权利人:CHEMO IBERICA SA 摘要:The invention is about a new synthetic pathway for the preparation of enantiomerically pure nitrogen substituted cyclopropanes, in particular the trans- cyclopropanamine ( 1 ), a key intermediate in the synthesis of Ticagrelor:n n The invention also relates to the processes for preparing said compounds or their salts and the use of said compounds as intermediates in preparing pharmaceutically active ingredients.
专利号:US-2013184465-A1 优先权日:2010-09-30 标 题:Process for the synthesis of thio-triazolo-group containing compounds 发明人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL 权利人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL; BASF SE 摘要:The present invention relates to a process using specific magnesium reagents for providing thio-triazolo group-containing compounds and for the synthesis of precursors therefor. The invention furthermore relates to intermediates and to their preparation.
专利号:US-5663046-A 优先权日:1994-06-22 标 题:Synthesis of combinatorial libraries 发明人:BALDWIN JOHN J; HORLBECK ERIC G 权利人:PHARMACOPEIA INC 摘要:Directly dividing the contents of each sub-pool into the sub-pools for the next step in the synthetic scheme for producing a combinatorial library reduces the standard deviation, sigma , relative to the standard deviation of the split synthesis method for producing such libraries.
专利号:US-8552175-B2 优先权日:2009-04-23 标题:Sulfur transfer reagents for oligonucleotide synthesis 发明人:GUZAEV ANDREI P 权利人:GUZAEV ANDREI P; A M CHEMICALS INC 摘要:The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones, 5-phenyl-3H-1,2,4-dithiazole-3-thiones, and derivatives thereof as novel, efficient sulfur-transfer reagents is disclosed. Sulfur transfer from these reagents to compounds containing a P(III) atom (e.g., triphenylphosphine, 5′-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5′-O-DMT-3′-O-levulinyl dithymidilyl 2-cyanoethyl phosphite), was studied in solution by 31 P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2′-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods. As opposed to many sulfur transfer reagents known in the prior art such as 1,2-benzodithiol-3-one-1,1-dioxide (Beaucage reagent) and 5-ethoxy-3H-1,2,4-dithiazole-2-one (EDIT), the sulfurizing agents disclosed herein are highly stable in solution, which increases their practical and commercial value.