专利号:US-2022267266-A1 优先权日:2019-07-09 标 题 :Improved, cost effective process for synthesis of vitamin d3 and its analogue calcifediol from ergosterol 发明人:DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; PRABHU MANOJKUMAR SADANAND; KADAM SACHIN VASANT 权利人:FERMENTA BIOTECH LTD 摘要:Disclosed herein is an improved and efficient process for synthesis of vitamin D3 and its analogue Calcifediol from Ergosterol. Particularly, the present invention discloses the synthesis of key intermediate 3β-tert-Butyldimethylsilyloxy-22-hydroxy-23,24-bisnorchola-5,7-diene (5), and novel intermediate β-tert-Butyldimethylsilyloxy-22-iodo-23,24-bisnorchola-5,7-diene (9) by a simple and cost effective process. The industrially viable processes for preparation of said intermediate(s) results in providing provitamins with various side chains and the desired products in high yield.
专利号:WO-2023000636-A1 优先权日:2021-07-20 标题:Method for synthesis of (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate 发明人:LIU YANG; WEI YUANBO; WANG QIUFENG; Xue Duoqing; WU YONG 权利人:ACCELA CHEMBIO CO LTD 摘要:A method for synthesis of (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate. A target product is prepared by using diethyl 2-fluoromalonate as a raw material and by means of a methylolation reaction, a hydroxyl protection reaction, a reduction reaction, an esterification reaction, a deprotection reaction, and a ring closure reaction in six steps. The steps are simple, the operation is easy, the raw material utilization rate and the product yield are high, intermediates are easy to separate, and the method is suitable for industrial scale-up production in terms of process safety, cost, raw material utilization rate, product purity, and the like. The results of embodiments show that the total yield of the reactions in the six steps of the method is 40-60%, and the HPLC purity of the target product (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate is greater than 97%.
专利号:EP-2017267-A1 优先权日:2007-07-16 标 题:Synthesis of statins 发明人:KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ 权利人:LEK PHARMACEUTICALS 摘要:The process for synthesis of statins is presented where the intermediate intermediate (4 R ,6 S )-6-(dialkoxymethyl)tetrahydro-2 H -pyran-2,4-diol which already possesses the desired stereochemistry corresponding to final statin is prepared by an aldolaze.
专利号:US-8471045-B2 优先权日:2007-04-03 标题 :Synthesis of statins 发明人:CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ 权利人:CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ; LEK PHARMACEUTICALS 摘要:The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.
专利号:US-10226434-B2 优先权日:2015-01-30 标题:Design, synthesis and methods of use of acyclic fleximer nucleoside analogues having anti-coronavirus activity 发明人:RADTKE KATHERINE L; PETERS HANNAH; NEYTS JOHAN; JOCHMANS DIRK; SNIJDER ERIC J 权利人:UNIV MARYLAND; KATHOLIEKE UNIV LEUVEN/LIEDEN UNIV MEDICAL CENTER RC LEIDEN 摘要:The present invention is directed to compounds, methods and compositions for treating or preventing viral infections using nucleosides analogs. Specifically, the present invention provides for the design and synthesis of acyclic fleximer nucleoside analogues having increased flexibility and ability to alter their conformation structures to provide increased antiviral activity potential with the result of inhibiting several coronaviruses.
专利号:US-9255119-B2 优先权日:2009-07-31 标 题:Process for perparing fondaparinux sodium and intermediates useful in the synthesis thereof 发明人:NADJI SOURENA; SMOOT JAMES T; VANARTSDALEN JOSEPH A 权利人:RELIABLE BIOPHARMACEUTICAL CORP 摘要:Processes for the synthesis of the Factor Xa anticoagulent Fondaparinux, and related compounds are described. Also described are protected pentasaccharide intermediates as well as efficient and scalable processes for the industrial scale production of Fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions.