专利号:EP-1721894-A1 优先权日:2005-05-13 标题 :Process for the synthesis of prostaglandin derivatives 发明人:LISI GIUSEPPE 权利人:TECHNOPHARMA SA 摘要:An alternative method for the synthesis of prostaglandin F analogues, in particular, analogues of PGF 2α and specifically for the synthesis of latano-prost, wherein the transformation of the lactone intermediate (5)n ninto the corresponding lactol (7)n nis carried out by treating the lactone intermediate (5) with a silane, preferably polymethylhydrosiloxane (PMHS), in the presence of a titanocene - and preferably titanocene fluoride. n The method enables considerable production economies with respect to the conventional reduction of lactone with diisobutylaluminum hydride (DIBAL-H).
专利号:US-7157590-B2 优先权日:2001-05-31 标题 :Process for the preparation of 17-phenyl-18,19,20-thinor-pgf 2a and its derivatives 发明人:GUTMAN ARIE; NISNEVICH GENNADY; ETINGER MARINA; ZALTZMAN IGOR; YUDOVITCH LEV; PERTSIKOV BORIS 权利人:FINETECH LAB LTD 摘要:The present invention provides a new and effective process for the synthesis of 17-phenyl-18,19,20-trinor-PGF 2α and its derivatives, including the anti-glaucoma drugs Bimatoprost and Latanoprost. The benefit of the present invention rises inter alia from the fact that a major intermediate involved in the synthesis of the above compounds may be isolated from a mixture containing also an undesired isomer, by crystallization. In addition, the undesired isomer may be oxidized to give the starting compound, which is then recycled.
专利号:EP-0495069-B1 优先权日:1990-08-08 标题:A method for synthesis of prostaglandin derivatives 发明人:RESUL BAHRAM 权利人:PHARMACIA AB 摘要:Method for preparing 13,14-dihydro-17-phenyl analogues of PGF2 alpha or PGE2 comprising the step of hydrogenating the double bond in an intermediate compound (I) without deoxygenation of the allylic alcohol to give one of the intermediate compounds (II, III) wherein R is hydrogen or one or more halogen, hydroxyl, cyanide, alkyl (preferably 1-4 carbon atoms), hydroxyalkyl, trifluoromethyl or aromatic or heteroaromatic substituents on the aromatic ring R1 and R2 are each hydrogen, alkyl (preferably 1-4 carbon atoms), hydroxyl, halogen or hydroxyalkyl substituents, R3 is O-alkyl or N(alkyl), P is a protecting group.
专利号:US-5359095-A 优先权日:1990-08-08 标 题:Method for synthesis of prostaglandin derivatives 发明人:RESUL BAHRAM 权利人:PHARMACIA AB 摘要:##STR1## Method for preparing 13,14-dihydro-17-phenyl analogues of PGF 2 α or PGE 2 comprising the step of hydrogenating the double bond in an intermediate compound (1) without deoxygenation of the allylic alcohol to give one of the intermediate compounds (II, III) wherein R is hydrogen or one or more halogen, hydroxyl, cyanide, alkyl (preferably 1-4 carbon atoms). hydroxyalkyl, trifluoromethyl or aromatic or heteroaromatic substituents on the aromatic ring R 1 and R 2 are each hydrogen alkyl (preferably 1-4 carbon atoms), hydroxyl, halogen or hydroxyalkyl substituents, R 3 is O-alkyl or N(alkyl), P is a protecting group.
专利号:RU-2073668-C1 优先权日:1990-08-08 标 题 :METHOD OF SYNTHESIS OF 13,14-DIHYDRO-17-PHENYL ANALOG OF PGF2α OR PGF2
专利号:US-7498458-B2 优先权日:2001-05-24 标 题 :Process for the preparation of prostaglandins and analogues thereof 发明人:GREENWOOD ALAN KENNETH; MCHATTIE DEREK; THOMPSON DAVID GEORGE; CLISSOLD DEREK 权利人:RESOLUTION CHEMICALS LTD 摘要:Disclosed are processes for the synthesis and purification of prostaglandins and analogues thereof, especially analogues of PGF2alpha.
参考标题:A Facile And Efficient Synthesis Of (15R)-Latanoprost From Chiral Precursor Corey Lactone Diol 作者:K Vijendhar,B Srinivas,Sathyanarayana Boodida |发布日期:2015.11 摘要:Synthetic Protocol Is A Good Alternative For The Synthesis Of Latanoprost With High Stereo Selectivity And Improved Yield. A Simple, Convenient And Convergent Approach For The Synthesis Of (15R) Latanoprost Is Reported With High Stereo Selectivity And Improved Yield From Chiral Precursor Corey Lactone Diol Using Swern Oxidation, Allylic Reduction And Wittig Reaction Conditions.