专利号:US-7125983-B2 优先权日:2000-11-29 标题:L-nucleic acid derivatives and process for the synthesis thereof 发明人:IIZUKA HAJIME; TOGASHI KAZUHIKO; SUZUKI TSUNEJI 权利人:MITSUI CHEMICALS INC 摘要:A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. A novel method has been further found to L-2′-deoxyribose derivatives as a useful synthetic intermediate through L-2,2′-anhydro-5,6-dihydrocyclouridine derivative. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now.
专利号:US-2005014954-A1 优先权日:2001-11-22 标 题:Pyrrole synthesis 发明人:OHRLEIN REINHOLD; BAISCH GABRIELE 摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.
专利号:US-8026383-B2 优先权日:2001-07-06 标题:Process for the preparation of intermediates useful in the synthesis of statin derivatives 发明人:OEHRLEIN REINHOLD; BAISCH GABRIELE; END NICOLE; BURKHARDT STEPHAN; STUDER MARTIN 权利人:BASF SE 摘要:The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I n nwherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH 3 )OCH 3 , R a is a hydroxy-protecting group and R b is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
专利号:US-2005176941-A1 优先权日:2002-02-13 标 题:Nucleoside analogues whose sugar moieties are bound in s-form and oligonucleotide derivatives comprising nucleotide analogues thereof 发明人:IMANISHI TAKESHI; OBIKA SATOSHI 摘要:Compounds of the following general formula (1) and salts thereof: n n nwhere A represents an alkylene group having 1 to 2 carbon atoms, etc.; B represents an aromatic heterocyclic group which may have a substituent, etc.; R 1 and R 2 each represent a hydrogen atom, a protective group for a hydroxyl group for synthesis of nucleic acid, a phosphate group, or —P(R 4 )R 5 [where R 4 and R 5 are the same or different, and each represent a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, a mercapto group, a mercapto group protected with a protective group for synthesis of nucleic acid, etc.]; and R 3 represents a hydrogen atom, a halogen atom, a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, etc. nThese compounds are useful for producing oligonucleotide analogues useful for the antisense method, antigene method, etc., and for producing their intermediates.
专利号:US-11225655-B2 优先权日:2010-04-16 标题:Bi-functional complexes and methods for making and using such complexes 发明人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK 权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS 摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.
专利号:US-7692034-B2 优先权日:2001-07-06 标题:Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives 发明人:OEHRLEIN REINHOLD; BAISCH GABRIELE; KIRNER HANS JUERG; BIENEWALD FRANK; BURKHARDT STEPHAN; STUDER MARTIN 权利人:TEVA PHARMA 摘要:The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein R a and R c are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and R b is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein R a and R c are each independently of the other hydrogen or a hydroxy-protecting group, and R b is a carboxy-protective group.