专利号:US-7897758-B2 优先权日:2005-04-27 标题 :Activators for oligonucleotide and phosphoramidite synthesis 发明人:WOLTER ANDREAS; LEUCK MICHAEL 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel methods for the synthesis of oligonucleotides and nucleoside phosphoramidites. The methods are based on employing aryl-substituted 5-phenyl-1H-tetrazoles with perfluoroalkyl groups on the aromatic ring as activators. In one aspect the novel activators are used in the synthesis of oligonucleotides via the phosphoramidite approach. In this aspect the activators are highly efficient and can be applied with very short coupling times. In a further aspect, the activators of the invention are used in the synthesis of phosphoramidites through the reaction of nucleosides comprising a free hydroxyl group with phosphitylating agents. In this aspect the activators provide very pure phosphoramidites under mild conditions. The activators of the invention are further characterized by being highly soluble, non-hygroscopic and non-hazardous.
专利号:US-4822903-A 优先权日:1981-05-15 标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof 发明人:JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT 权利人:RHONE POULENC SPEC CHIM 摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.
专利号:US-5254558-A 优先权日:1991-08-15 标 题:Substituted 1,3-diazines as leukocyte elastase inhibitors 发明人:BERNSTEIN PETER R; EDWARDS PHILIP D; THOMAS ROYSTON M; VEALE CHRIS A; WARNER PETER; WOLANIN DONALD J 权利人:ICI PLC 摘要:The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
专利号:US-9550757-B2 优先权日:2010-03-05 标题:Nuclear transport modulators and uses thereof 发明人:SHACHAM SHARON; KAUFFMAN MICHAEL; SANDANAYAKA VINCENT P; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
专利号:US-9714226-B2 优先权日:2011-07-29 标题:Hydrazide containing nuclear transport modulators and uses thereof 发明人:SANDANAYAKA VINCENT P; SHACHAM SHARON; MCCAULEY DILARA; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: n nor a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
专利号:US-9428490-B2 优先权日:2011-07-29 标 题 :Nuclear transport modulators and uses thereof 发明人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD 权利人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD; KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
参考标题:Cobalt-Catalyzed Electrophilic Cyanation Of Arylzinc Halides WithN-Cyano-N-Phenyl-P-Methylbenzenesulfonamide (Ncts) 作者:Yingxiao Cai,Xin Qian,Alice Rérat,Audrey Auffrant,Corinne Gosmini |发布日期:2015.11.16 摘要:The Cobalt-Catalyzed Cross-Coupling Of Organozinc Bromides With N-Cyano-N-Phenyl-P-Methylbenzenesulfonamide (Ncts) Is Described. The Same Cobalt Catalyst, Cobalt(II) Bromide, Was Used For Both The Synthesis Of The Organozinc Species And The Cross-Coupling Reaction. However In This Case, A Catalytic Amount Of Zinc Dust Is Necessary In The Second Step To Release The Low-Valent Cobalt. Under These Mild
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摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 388.