专利号:US-7247752-B2 优先权日:2004-10-01 标 题 :Methods for the synthesis of astaxanthin 发明人:LOCKWOOD SAMUEL F; TANG PENG CHO; NADOLSKI GEOFF; JACKSON HENRY L; FANG ZHIQIANG; DU YISHU; YANG MIN; GEISS WILLIAM; WILLIAMS RICHARD; BURDICK DAVID 权利人:CARDAX PHARMACEUTICALS INC 摘要:A method used for synthesizing intermediates for use in the synthesis of carotenoids and carotenoid analogs, and/or carotenoid derivatives. In some embodiments, the invention includes methods for synthesizing optically active intermediates useful for the synthesis of optically active carotenoids. Synthesis of optically active carotenoids, in one embodiment, may be accomplished by forming an optically active dihydroxy intermediate from ketoisopherone. The optically active dihydroxy intermediate may be converted into optically active astaxanthin derivatives.
专利号:US-5932726-A 优先权日:1996-12-16 标 题 :Asymmetric synthesis of benzoxazinones 发明人:PIERCE MICHAEL ERNEST; CHOUDHURY ANUSUYA; PARSONS JR RODNEY LAWRENCE; RADESCA LILIAN ALICIA 权利人:DU PONT PHARM CO 摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
专利号:US-6040480-A 优先权日:1997-04-07 标题 :Asymmetric synthesis of benzoxazinones 发明人:PIERCE MICHAEL E; CHEN CHENG Y; CHOUDHURY ANUSUYA; RADESCA LILIAN A; TAN LUSHI; ZHAO DALIAN 权利人:DU PONT PHARM CO 摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
专利号:US-5856492-A 优先权日:1997-01-10 标题 :Efficient synthesis of a chiral mediator 发明人:CHEN CHENG YI; XU FENG; TILLYER RICHARD D; ZHAO DALIAN 权利人:MERCK & CO INC 摘要:An efficient method for the quantitative preparation and isolation of a compound of formula I ##STR1## or its enantiomer, a chiral mediator used in enantioselective synthesis.
专利号:US-5962737-A 优先权日:1997-01-08 标 题 :2-amino-1-phenylpropanols, stereospecific synthesis thereof, and method of optically resolving the same 发明人:WEST DANIEL DAVID 摘要:Stereospecific synthesis of the racemic threo isomers of 2-nitro-1-phenylpropanols by reacting a benzaldehyde derivative with nitroalkane in the presence of a tertiary amine and reducing 2-nitro-1-phenylpropanols with, for example, lithium aluminum hydride to 2-amino-1-phenylpropanols is described. Also described are phase transfer resolution of racemic mixtures of 2-amino-1-phenylpropanol and its derivatives into their optically pure isomers by reacting a racemic mixture with the mono alkali metal salt of a tartaric acid ester in a two phase system of a hydrocarbon and water. The specification further describes therapeutically useful optically pure isomers of threo-2-amino-1-(dialkoxy or alkoxy) phenylpropanols and acid addition salts thereof.
专利号:US-2004110957-A1 优先权日:2002-12-05 标 题 :Process for the synthesis of an antiviral compound 发明人:WILKEN JOERG; NERENZ FRANK; KANSCHIK-CONRADSEN ANDREAS 权利人:HONEYWELL INT INC 摘要:In a process comprising synthesizing pyranes including [R—(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide the present invention comprises the improvements comprising: (a) providing a racemic mixture of 3-hydroxy-3-(2-phenylethyl)-hexanoate ethyl acetate by reacting said 1-phenyl-hexan-3-one with ethylbromoacetate under Reformatsky conditions; and (b) separating (R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid in enantiomeric excess by saponification and reverse resolution of the racemate of step (a) to produce a resolved product. In addition, the present invention comprises a reverse resolution process for separating an enantiomer from a mixture of enantiomers.
参考文献:10.2165/11530130-000000000-00000 摘要:Hasnain M, Vieweg WV, Fredrickson SK. Metformin for atypical antipsychotic-induced weight gain and glucose metabolism dysregulation: review of the literature and clinical suggestions. CNS Drugs. 2010 Mar;24(3):193–206. doi: 10.2165/11530130-000000000-00000. 参考文献:10.1007/s00467-011-1964-0 摘要:Chandar J, Zilleruelo G. Hypertensive crisis in children. Pediatr Nephrol. 2012 May;27(5):741–51. doi: 10.1007/s00467-011-1964-0.