专利号:US-5948789-A 优先权日:1994-07-15 标题:Process for synthesis of substituted sulphoxides 发明人:LARSSON MAGNUS ERIK; STENHEDE URBAN JAN; SOERENSEN HENRIK; VON UNGE SVERKER PER OSKAR; COTTON HANNA KRISTINA 权利人:ASTRA AB 摘要:PCT No. PCT/SE95/00818 Sec. 371 Date Jul. 14, 1995 Sec. 102(e) Date Jul. 14, 1995 PCT Filed Jul. 3, 1995 PCT Pub. No. WO96/02535 PCT Pub. Date Feb. 1, 1996A novel process for enantioselective synthesis of single enantiomers of omeprazole or its alkaline salts, of other optically pure substituted 2-(2-pyridinylmethyl-sulphinyl) -1H-benzimidazoles as well as of other structurally related sulphoxides or their alkaline salts. The claimed process is an asymmetric oxidation of a pro-chiral sulphide to the single enantiomers or an enantiomerically enriched form of the corresponding sulphoxide. The application also claims the enantiomeric sulphoxide products produced by the process and their use in medicine.
专利号:US-8697880-B2 优先权日:2004-02-20 标 题 :Compounds useful for the synthesis of S- and R-omeprazole and a process for their preparation 发明人:VON UNGE SVERKER; FREGLER CHRISTINA 权利人:UNGE SVERKER VON; FREGLER CHRISTINA; ASTRAZENECA AB 摘要:The present invention relates to an improved method for the synthesis of the (S)- or (R)-enantiomer of omeprazole, characterized in that 2-[[(4-X-3,5-dimethylpyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole or 2-[[(4-X-3,5-dimethyl-1-oxidopyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole, wherein X is a leaving group, is oxidized into the corresponding sulphoxide which is obtained as a crystalline compound. Recrystallization of the thus obtained sulphoxide results in a compound of enhanced chemical and optical purity, which is subsequently transformed into the (S)- or (R)-enantiomer of omeprazole.
专利号:US-5702928-A 优先权日:1994-07-18 标题 :Process for producing optically active triazole compounds and method of racemizing optically active triazole compounds 发明人:KAWADA NAOKI; YAMAZAKI NORITSUGU; IMOTO TAKAFUMI; IKURA KIYOSHI 权利人:DAICEL CHEM 摘要:PCT No. PCT/JP95/01416 Sec. 371 Date May 24, 1996 Sec. 102(e) Date May 24, 1996 PCT Filed Jul. 17, 1995 PCT Pub. No. WO96/02664 PCT Pub. Date Feb. 1, 1996A process for the asymmetric synthesis of a compound represented by general formula (II-R) easily at a low cost by using a lipase, and a process for producing a compound to be utilized in the above synthesis. (II-R)
专利号:US-11365211-B2 优先权日:2018-02-01 标 题 :Stereoselective synthesis and process for the manufacturing of 2′-deoxynucleosides 发明人:ZHANG LIANHAO; VISHNUVAJJALA BABURAO; MORRIS JOEL; BAHDE ROBERT; DENYSENKO SERGIY M; LOPEZ OMAR DIEGO; WISHKA DONN GREGORY 权利人:THE USA AS REPRESENTED BY THE SEC DEP OF HEALTH AND HUMAN SERVICES; ALCHEM LABORATORIES CORP; US HEALTH 摘要:Methods for stereoselective synthesis and manufacturing of 2′-deoxynucleosides, such as 2′-ribonucleosides, are disclosed. In some embodiments, the 2′-deoxynucleoside is a β-anomer of a 2′-deoxynucleoside having a 3′ α hydroxyl, 4′ β hydroxymethyl configuration. Nonlimiting examples of compounds prepared by the disclosed methods include 4′-thio-2′-deoxycytidine (T-dCyd) and 5-aza-4′-thio-2′-deoxycytidine (5-aza-T-dCyd; aza-T-dCyd; aza-T-dC).
专利号:US-7915422-B2 优先权日:2004-10-11 标题:Processes for the preparation of substituted sulfoxides 发明人:KUMAR NEELA PRAVEEN; KHANNA MAHAVIR SINGH; PRASAD MOHAN; KUMAR YATENDRA 权利人:RANBAXY LAB LTD 摘要:The present invention relates to a process for enantioselective synthesis of substituted pyridinylmethyl sulfinyl-benzimidazole of compound of Formula (I). The process includes enantioselective catalytic oxidation of a substituted pyridinylmethyl prochiral sulfide derivative of compound of Formula (II) with an oxidizing agent in the presence of a chiral transition metal complex and a base in the absence of an organic solvent.
专利号:US-7393954-B2 优先权日:2002-12-12 标题:Process for the production of pentostatin aglycone and pentostatin 发明人:NADJI SOURENA; SMOOT JAMES; SAMPATH UMASHANKER 权利人:RELIABLE BIOPHARMACEUTICAL COR 摘要:A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates.
参考标题:Stereocontrolled Total Synthesis Of The Macrocyclic Lactone (−)-Aspicilin 作者:P.P. Waanders,L. Thijs,B. Zwanenburg 摘要:The Essential Features Of The Enantiocontrolled Total Synthesis Of (−)-Aspicilin Are The Strategic Use Of The Photochemical Rearrangement Of α,β-Epoxy Diazomethyl Ketones To 4-Hydroxyalkenoates (Scheme 1) And The Stereochemical Control Of The Sharpless Epoxidation, α,ω Functionalization Of An Alkynol Using Potassium 3-Aminopropylamine (Kapa) As Acetylene Zipper, Coupling Between C7 And C8 By Means
合成参考文献
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