专利号:US-12037623-B2 优先权日:2018-07-09 标 题 :Enzymatic synthesis of 4′-ethynyl nucleoside analogs 发明人:HUFFMAN MARK A; FRYSZKOWSKA ANNA; KOLEV JOSHUA N; DEVINE PAUL N; CAMPOS KEVIN R; TRUPPO MATTHEW; NAWRAT CHRISTOPHER C 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC 摘要:The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.
专利号:US-8168556-B2 优先权日:2007-10-25 标 题 :Racemoselective synthesis of ansa-metallocene compounds, ansa-metallocene compounds, catalysts comprising them, process for producing an olefin polymer by use of the catalysts, and olefin homo- and copolymers 发明人:SCHULTE JOERG; SELL THORSTEN; THORN MATTHEW GRANT; WINTER ANDREAS; DIMESKA ANITA 权利人:SCHULTE JOERG; SELL THORSTEN; THORN MATTHEW GRANT; WINTER ANDREAS; DIMESKA ANITA; LUMMUS NOVOLEN TECHNOLOGY GMBH 摘要:A metallocene compound with the 4- and 7-positions on the indenyl moiety possessing large aromatic substituents is prepared in accordance with a method which produces substantially 100 percent racemic isomer. Advantageously, polymerization catalysts including the metallocene of the invention provide superior olefin polymerization results.
专利号:US-3862978-A 优先权日:1967-08-24 标 题:Catalytic synthesis of organic halogen compounds from an ethylenically unsaturated compound and a halogenated organic compound 发明人:DECKER DALTON L; MOORE CARL; TOUSIGNANT WILLIAM F 权利人:DOW CHEMICAL CO 摘要:Method for forming a chemical adduct of an ethylenically unsaturated compound with a halogenated organic compound having on a single carbon atom thereof at least two halogen atoms at least one of which is chlorine, bromine or iodine, characterized by employing a catalyst of which the essential members are copper and an amine selected from piperidine, substituted piperidines, cyclohexylamines and secondary amines on which the hydrocarbyl substituents are allyl, benzyl or lower alkyl radicals.
专利号:US-5859190-A 优先权日:1997-02-04 标题 :Combinatorial libraries of hydantoin and thiohydantoin derivatives, methods of making the libraries and compounds therein 发明人:MEYER JEAN-PHILIPPE; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of hydantoin and thiohydantoin compounds. The present invention further provides the compounds made by the combinatorial synthesis.
专利号:US-9809591-B2 优先权日:2011-03-08 标题 :Heterocyclic modulators of lipid synthesis 发明人:OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W 权利人:3-V BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
专利号:US-6013838-A 优先权日:1998-01-27 标题:Chemical intermediates bearing a trifluoromethyl group 发明人:VAN DER PUY MICHAEL 权利人:ALLIED SIGNAL INC 摘要:Novel trifluoromethylated intermediates are provided which are useful in synthesizing trifluoromethylated organic compounds. Specifically, compounds of the formula CF 3 CR are provided, wherein R is (Cl)â•?CHCH 2 SO 2 Ph, (Cl)â•?CHCH 2 CH 2 C(â•?O)CH 3 , (Cl)â•?CHCH 2 CH(COCH 3 ) 2 , (Cl)â•?CHCH 2 NR'R' or Hâ•?CHCHâ•?NR'; R' and R' are the same or different and are selected from the group consisting of hydrogen, unsubstituted or substituted C 1 to C 6 straight chain or branched alkyl, unsubstituted or substituted C 3 to C 7 cycloalkyl, unsubstituted or substituted C 2 to C 12 alkenyl, a benzyl group unsubstituted or substituted with R'', or a phenyl group unsubstituted or substituted with R''; or R' and R' taken together form a five- or six-membered ring; and R'' is an unsubstituted or substituted C 1 to C 6 straight chain or branched alkyl, an unsubstituted or substituted C 1 to C 6 alkoxy, an unsubstituted or substituted C 1 to C 6 thioakyl, a cyano, a halogen, or a C 1 to C 2 dialkylamino group; with the proviso that when the alkyl, cycloalkyl or alkenyl of R' or R' or the alkyl, alkoxy or thioalkyl of R'' is substituted, it may be substituted with any group compatible with amine functionality. The novel compounds are versatile intermediates for the synthesis of a wide variety of trifluoromethylated organic compounds, which have found great utility as pharmaceuticals, agricultural chemicals, and materials such as liquid crystals.
摘要:Beccalli, E. M.; Bonetti, A.; Mazza, A., Science of Synthesis: Metal-Catalyzed Cyclization Reactions, (2016) 1, 445. 摘要:W. H. Carothers, C. F. Bickford, and G. J. Hurwitz. J. Am. Chem. Soc. 49, 2908 (1927).