专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:US-4751312-A 优先权日:1984-07-20 标 题:Process and intermediates for the synthesis of diastereomeric compounds 发明人:GASTEIGER JOHANN; KAUFMANN KARLHEINZ; MENGEL RUDOLF 权利人:BAYER AG 摘要:A new process for the controlled synthesis of the two diasteromeric forms of triazolyl-O,N-acetals of the formula (I) in which R represents optionally substituted phenyl, optionally substituted phenoxy, optionally substituted alkoxy, optionally substituted alkoxy, optionally substituted alkylthio, alkylcarbonyl, nitro or halogen and n represents an integer from 0 to 5, with the proviso that R can represent identical or different radicals, if n represents an integer from 2 to 5. New trans-substituted oxiranes and their use as intermediates for the synthesis of compounds of the formula (I).
专利号:US-7122693-B2 优先权日:1988-04-11 标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof 发明人:BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE 权利人:SHIRE BIOCHEM INC 摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-12435042-B2 优先权日:2019-07-04 标题:Process for the preparation of key intermediates for the synthesis of Eltrombopag or salt thereof 发明人:STABILE PAOLO; SEMERARO FLORIANA 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of Eltrombopag, passing through/using intermediate 5′-Chloro-2′-hydroxy[1,1′-biphenyl]-3-carboxylic acid alkaline metal salt of formula: wherein A is an alkaline metal.
专利号:US-8283502-B2 优先权日:2009-04-09 标题:Autocatalytic process for the synthesis of chiral propargylic alcohols 发明人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK 权利人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK; LONZA AG 摘要:An autocatalytic process for the synthesis of chiral propargylic alcohols.