专利号:US-10266503-B1 优先权日:2016-05-24 标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins 发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN 权利人:UNIV ILLINOIS 摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.
专利号:US-8748459-B2 优先权日:2002-03-29 标 题 :Pyridinoylpiperidines as 5-HT1F agonists 发明人:COHEN MICHAEL PHILIP; KOHLMAN DANIEL TIMOTHY; LIANG SIDNEY XI; VICTOR FRANTZ; XU YAO-CHANG; YING BAI-PING; ZACHERL DEANNA PIATT; ZHANG DEYI 权利人:COHEN MICHAEL PHILIP; KOHLMAN DANIEL TIMOTHY; LIANG SIDNEY XI; VICTOR FRANTZ; XU YAO-CHANG; YING BAI-PING; ZACHERL DEANNA PIATT; ZHANG DEYI; LILLY CO ELI 摘要:The present invention relates to compounds of formula I: n nor pharmaceutically acceptable acid addition salts thereof, where;n R 1 is C 1 -C 6 alkyl, substituted C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, substituted C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkyl-C 1 -C 3 alkyl, substituted C 3 -C 7 cycloalkyl-C 1 -C 3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R 2 is hydrogen, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl-C 1 -C 3 alkyl, or a group of formula II nn n n n n n n n n n n n R 3 is hydrogen or C 1 -C 3 alkyl; n R 4 is hydrogen, halo, or C 1 -C 3 alkyl; n R 5 is hydrogen or C 1 -C 3 alkyl; n R 6 is hydrogen or C 1 -C 6 alkyl; and n n is an integer from 1 to 6 inclusively. n n n n n The compounds of the present invention are useful for activating 5-HT lF receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
专利号:US-2011301143-A1 优先权日:2009-02-23 标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ•?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
专利号:WO-2018191612-A1 优先权日:2017-04-14 标 题 :Synthesis of a phosphorous containing monomer and the incorporation in polycarbonate by interfacial polymerization thereof
专利号:US-6812320-B2 优先权日:2002-03-25 标题:Method for copolyestercarbonate synthesis 发明人:SILVA JAMES MANIO; DARDARIS DAVID MICHEL; O'NEIL GREGORY ALLEN; SYBERT PAUL DEAN; SU ZHAOHUI 权利人:GEN ELECTRIC 摘要:Thermally stable block copolyestercarbonates comprising chain members derived from at least one dihydroxy-substituted aromatic hydrocarbon moiety and at least one aromatic dicarboxylic acid moiety, said polymer being substantially free of anhydride linkages linking at least two mers of the polyester chain segments, are prepared by a method comprising the steps of: (a) preparing a hydroxy-terminated polyester intermediate comprising structural units derived from at least one dihydroxy-substituted aromatic hydrocarbon moiety and at least one aromatic dicarboxylic acid moiety; and (b) conducting a reaction of the polyester intermediate with phosgene in a reaction mixture comprising water, a substantially water-immiscible organic solvent, and a base, wherein base and phosgene are added simultaneously to the reaction mixture at a substantially constant molar ratio of base to phosgene for a time period of at least about 60% of the total amount of phosgene added.
专利号:US-2020048410-A1 优先权日:2017-04-14 标 题:Synthesis of a phosphorous containing monomer and the incorporation in polycarbonate by interfacial polymerization thereof