专利号:US-8404088-B2 优先权日:2006-05-22 标 题:Asymmetric synthesis of rocaglamides via enantioselective photocycloaddition mediated by chiral bronsted acids 发明人:PORCO JR JOHN A; GERARD BAUDOUIN 权利人:PORCO JR JOHN A; GERARD BAUDOUIN; UNIV BOSTON 摘要:The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
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.
专利号:US-7812193-B2 优先权日:2003-09-19 标题:Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation 发明人:REBIERE FRANCOIS; DURET GERARD; PRAT LAURENCE 权利人:CEPHALON FRANCE 摘要:The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of:n a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I); nn nwherein n, Y, R 1 , R 1a , R 2 and R 2a are as defined herein.
专利号:US-2005222257-A1 优先权日:2003-09-19 标题:Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation
专利号:US-7317126-B2 优先权日:2003-09-19 标 题:Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation
专利号:CA-2538697-C 优先权日:2003-09-19 标 题 :Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation
参考文献:10.1007/bf00563684 摘要:Berlin YA, Kolosov MN, Piotrovich LA. Olivomycin and related antibiotics XXVI. The absolute configurations of olivin and of chromomycinone. Chemistry of Natural Compounds. 1972 Jul;8(4):515–21. doi: 10.1007/bf00563684.