专利号:US-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
专利号:EP-1501848-B1 优先权日:2002-05-08 标 题 :Synthesis of locked nucleic acid derivatives 发明人:SORENSEN MADS DETLEF; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER 权利人:SANTARIS PHARMA AS 摘要:The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as alpha-L-oxy-LNA, amino-LNA, alpha-L-amino-LNA, thio-LNA, alpha-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. (Formula I)
专利号:US-7105666-B2 优先权日:2002-06-27 标 题:Synthesis of purine derivatives 发明人:HAMMARSTROEM LARS G J; KRAUSS NANCY ELISABTH; LABADIE SHARADA SHENVI; SMITH DAVID BERNARD; TALAMAS FRANCISCO XAVIER 权利人:ROCHE PALO ALTO LLC 摘要:The present invention provides a method for producing 2-, 6-, 8- and 9-substituted purine compounds from 4,6-dihalo-5-nitro-2-alkyl-pyrimidine compounds in solution or by solid phase techniques. The present process provides for the sequential introduction of amine substituents at the 4- and 6-positions, displacement of an alkylsulfony group at the 2-position of the pyrimidine, reduction of the nitro group and formation of the imidazole portion of the purine compound. Furthermore, the methods of the present invention are ideally suited to the preparation of a library of purine compounds.
专利号:US-7582748-B2 优先权日:2003-03-20 标题:Methods of manufacture of 2′-deoxy-β-L-nucleosides 发明人:RABI JAIME A 权利人:MICROBIOL QUIMICA FARMACEUTICA 摘要:The present invention relates to the synthesis of 2′-deoxy-β-L-thymidine, 2′-deoxy-β-L-uridine and 2′-deoxy-β-L-cytidine, and their derivatives, such as the 3′-O-acyl or 3′,5′-O-diacyl prodrugs, including the 3′-O-L-aminoacyl and 3′,5′-O-L-diaminoacyl prodrugs, and particularly the 3′-O-L-valinyl and 3′,5′-O-L-divalinyl prodrugs.
专利号:US-5401844-A 优先权日:1983-04-11 标 题 :Regulation of enzymes which utilize tetrahydrobiopterin or tetrahydrofolate cofactors with 6,6-disubstituted-tetrahydropteridines 发明人:AYLING JUNE E; BAILEY STEVEN W 权利人:UNIV SOUTH ALABAMA 摘要:6-[2'-Amino-2',2'-disubstituted-ethylamino]-pyrimidines of the structure: ##STR1## in which X=H, NH 2 or NO 2 , which are novel intermediates in the synthesis of quinoid 6,6-disubstituted-dihydro- and 6,6-disubstituted-tetrahydro-pteridines, are claimed.
专利号:EP-0609960-B1 优先权日:1989-09-15 标 题 :New N-heteroarylamide derivatives as inhibitors of acyl coenzyme A: cholestrol acyl transferase 发明人:MCCARTHY PETER A; HAMANAKA ERNEST S; WALKER FREDERICK J; CHANG GEORGE; TRUONG THIEN 权利人:PFIZER 摘要:Compounds of the formula the pharmaceutically acceptable salts thereof, wherein Q and R<1> are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.