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:US-6448425-B1 优先权日:2002-02-19 标题:Preparation of N-substituted aminoorganosilanes 发明人:GEDON STEVEN C; HALE MELINDA 权利人:CROMPTON CORP 摘要:A process is disclosed for the synthesis of N-cycloalkylaminoalkylsilanes, wherein the process comprises hydrogenating the corresponding N-arylaminoalkylsilanes in the presence of a catalytically effective amount of a supported or unsupported catalyst selected from the group consisting of palladium, platinum, nickel, rhenium, rhodium, ruthenium, copper chromite, and mixtures of the foregoing.
专利号:US-7465842-B2 优先权日:2004-08-26 标 题 :Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates 发明人:KUNG PEI-PEI; MARTINEZ CARLOS; TAO JUNHUA 权利人:AGOURON PHARMA 摘要:The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resolution, chemical esterification and chemical hydrolysis with inversion of 1-(2,6-dichloro-3-fluorophenyl)ethyl esters or stereoselective bio-reduction of 2,6-dichloro-3-fluoro-acetophenone with a biocatalyst such as an enzyme or a microorganism. The chiral (S)-enantiomer can be used in the synthesis of certain enantiomerically enriched, ether linked 2-aminopyridine compounds that potently inhibit auto-phosphorylation of human heptocyte growth factor receptor.
专利号:US-4546198-A 优先权日:1983-01-18 标 题 :Asymmetric synthesis of esters and acids 发明人:STOUTAMIRE DONALD W 权利人:SHELL OIL CO 摘要:Stereoisomerically-enriched esters are prepared by treating a non-symmetrical ketene with a racemic or chiral tertiary-base-substituted alkylcarbinol. Optional hydrolysis of the esters gives the corresponding optically-active carboxylic acids corresponding to the non-symmetrical ketene.
专利号:US-8377895-B2 优先权日:2008-07-10 标 题 :Cyclin-dependent protein kinases inhibitors of Scutellaria flavonoid organic amine derivatives, synthesis and use thereof 发明人:ZHANG SHIXUAN; BAO YONGMING; SUN YUMING; LI KANGJIAN; ZOU LIANG; MA JIGANG; SUN XIAODAN; SHANG HAIYAN; LI JING 权利人:ZHANG SHIXUAN; BAO YONGMING; SUN YUMING; LI KANGJIAN; ZOU LIANG; MA JIGANG; SUN XIAODAN; SHANG HAIYAN; LI JING 摘要:The present invention provides a series of cyclin-dependent protein kinases (Cdks) inhibitors, Scutellaria flavonoid organic amine derivatives, synthesis and use thereof. The preparation method is as follows: taking Baicalein (or Wogonin) from Scutellaria baicalensis as lead compound, mixting it with formaldehyde solution and organic amine compounds based on the molar ratio of 1:1-1.2:1-1.2, adding methanol of duplicate weight than baicalein and reacting at 50-70° C., filtering the sediment and washing and then drying so as to get the product with a content of not less than 97% (weight). Similar to Flavopiridol and P276-00, the activity of baicalein organic amine derivatives inhibiting Cdks has an increase of 50 times compared with that of Baicalin. It can selectively induce apoptosis of the proliferative phase cancer cells, which has scarcely any influence to the normal structure, and it belongs to anticancer drugs of cell cycle inhibitor kind. The product has a rich source of raw materials and has simple process, high purity, low cost, clear metabolic mechanism, high efficiency and low toxicity, which can be made into oral preparations or injections together with acid salts and is expected to become high efficient and low toxicity anti-cancer and AIDS drugs.
专利号:US-7459552-B2 优先权日:2003-05-28 标 题:Method for producing cyclic diamine derivative or salt thereof 发明人:SHIBUYA KIMIYUKI; OHGIYA TADAAKI; MIURA TORU 权利人:KOWA CO 摘要:The present invention is directed to a method for producing a cyclic diamine compound (3) or a salt thereof through the following scheme: n n(wherein Ar represents a phenyl group, a pyridyl group, or a pyrimidinyl group, any of which may have a substituent; X represents NH, S, or O; ring A represents a benzene ring or a pyridine ring, which may have a substituent; 1 represents an integer of 1 or 2; m represents an integer of 1 or 2; and n represents an integer of 1 to 6). The method enables synthesis of a cyclic diamine compound (3) or a salt thereof, which serves as an ACAT inhibitor, in an industrially useful manner.