专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
专利号:US-6451727-B2 优先权日:1997-11-12 标题:Catalysts for use in asymmetric synthesis comprising transition metals and chiral amine oxazolinyl ligands 发明人:ZHANG XUMU 权利人:PENN STATE RES FOUND 摘要:The invention is drawn to transition metal catalysts for the practical synthesis of important chiral molecules. The transition metal catalysts comprise chiral ligands based on chiral amine oxazolinyl ligands. The invention includes methods of making the catalysts, and methods of performing reactions using the catalysts.
专利号:US-6380416-B2 优先权日:1997-06-13 标题:Asymmetric synthesis catalyzed by transition metal complexes with rigid chiral ligands 发明人:ZHANG XUMU 权利人:PENN STATE RES FOUND 摘要:This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral bidentate phosphine ligands with cyclic ring structures which could be used to restrict conformational flexibility of the ligands and thus the efficiency of chiral transfer can be enhanced through the ligand rigidity.
专利号:US-8350042-B2 优先权日:2008-01-31 标题 :Antiviral compounds for the treatment of HCV infection 发明人:HERMANN THOMAS C; CARNEVALI MAIA 权利人:UNIV CALIFORNIA; HERMANN THOMAS C; CARNEVALI MAIA 摘要:Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection.
专利号:US-5097051-A 优先权日:1989-02-10 标题 :Cyclic triketone compounds and trimethylsilyloxy butadiene compounds and their use in the preparation of daunomycinone derivatives 发明人:SCHEEREN JOHAN W; DEBIE JOANNES F M; DEVOS DIRK 权利人:PHARMACHEMIE BV 摘要:The invention provides novel cyclic triketone compounds of the formulae wherein S is H, alkyl or alkoxy and R* is a group of the formule wherein R<1> is methyl and R2 is an alkyl group containing at least 2 carbon atoms, or R<1> is an alkyl group having 1-4 carbon atoms and R<2> is an aryl group, a hetero aryl group, a -CH2OR min , a -CH2N @@ group, a -CH2SR sec group or a -CH2CH=CH2 group, wherein R min and R sec are alkyl groups having 1-4 carbon atoms. These compounds can be used for preparing daunomycinone and derivatives thereof. Daunomycinone is used for preparing daunomycin and adriamycin. By introducing chirality at C-1 of ring A in the preparation of said novel compounds by using a novel diene of formula (1) in a Diels-Alder reaction for said preparation, the chirality of C-3 is established in the subsequent reaction with LiC IDENTICAL CSi(CH3)3 in the synthesis of daunomycinone and derivatives thereof. This last reaction leads to the desired compound wherein OH at C-3 and OR at C-1 are in the cis-position with respect to each other.
专利号:US-5183913-A 优先权日:1989-02-10 标 题 :Cyclic triketone compounds and trimethylsilyoxy butadiene compounds and their use in the preparation of daunomycinone derivatives 发明人:SCHEEREN JOHAN W; MARTINUS DE BIE JOANNES F; DE VOS DIRK 权利人:PHARMACHEMIE BV 摘要:The invention provides novel cyclic triketone compounds of the formulae (2) (3) wherein S is H, alkyl or alkoxy and R* is a group of the formule wherein R1 is methyl and R2 is an alkyl group containing at least 2 carbon atoms or R1 is an alkyl group having 1-4 carbon atoms and R2 is an aryl group, a hetero aryl group, a -CH2OR' group, a -CH2N (1) This last reaction leads to the desired compound wherein OH at C-3 and OR at C-1 are in the cis-position with respect to each other.