- Copper-Catalyzed Oxidative Difunctionalization of Terminal Unactivated Alkenes
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The copper(II)-promoted free-radical oxidative difunctionalization of terminal alkenes to access ketoazides by utilizing molecular oxygen has been reported. A series of styrene derivatives have been evaluated and were found to be compatible to give the desired difunctionalized products in moderate to good yields. The role of molecular oxygen both as an oxidant and oxygen atom source in this catalytic transformation has been unquestionably demonstrated by 18O-labeling studies and a radical mechanistic pathway involving the oxidative formation of azidyl radicals is also designed. This environment-friendly catalytic oxidative protocol can transform aldehyde to nitrile.
- Hussain, Muhammad Ijaz,Feng, Yangyang,Hu, Liangzhen,Deng, Qingfu,Zhang, Xiaohui,Xiong, Yan
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supporting information
p. 7852 - 7859
(2018/05/30)
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- Pd-Catalyzed, ortho C-H Methylation and Fluorination of Benzaldehydes Using Orthanilic Acids as Transient Directing Groups
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The direct, Pd-catalyzed ortho C-H methylation and fluorination of benzaldehydes have been accomplished using commercially available orthanilic acids as transient directing groups. In these reactions, the 1-fluoro-2,4,6-trimethylpyridinium salts can be either a bystanding F+ oxidant or an electrophilic fluorinating reagent. An X-ray crystal structure of a benzaldehyde ortho C-H palladation intermediate was obtained using triphenylphosphine as the stabilizing ligand.
- Chen, Xiao-Yang,Sorensen, Erik J.
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supporting information
p. 2789 - 2792
(2018/03/08)
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- Regioselective routes to orthogonally-substituted aromatic MIDA boronates
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A series of tetrasubstituted aromatics has been synthesized, many of which are based on elaborated N-methyliminodiacetic acid (MIDA)-boronates. A sequence employing nitration, bromination, stepwise Suzuki-Miyaura (SM) coupling with a boronic acid, then base-mediated unmasking of the boronic acid from the MIDA-boronate and a second SM-coupling has led to our desired, mainly 1,2,4,5-substituted tetrasubstituted aromatic targets.
- Close, Adam J.,Kemmitt, Paul,Mark Roe,Spencer, John
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p. 6751 - 6756
(2016/07/21)
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- Preparation method of 2-fluoro-5-bromobenzaldehyde
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The invention relates to a preparation method of 2-fluoro-5-bromobenzaldehyde as a medicine intermediate. O-fluorobenzaldehyde and a bromination reagent undergo a reaction in the presence of Lewis acid as a catalyst and the reaction product is subjected to reduced pressure distillation so that 2-fluoro-5-bromobenzaldehyde with a high yield and high content is obtained. The preparation method has the characteristics of easy availability of raw materials, less reaction processes, high yield and low cost.
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Paragraph 0008; 0009; 0010; 0011
(2018/02/04)
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- ANILINE DERIVATIVES,THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
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The present invention relates to aniline derivatives, to their preparation and to their therapeutic application.
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Page/Page column 209; 210
(2013/03/28)
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- Fragment-based discovery of JAK-2 inhibitors
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Fragment-based hit identification coupled with crystallographically enabled structure-based drug design was used to design potent inhibitors of JAK-2. After two iterations from fragment 1, we were able to increase potency by greater than 500-fold to provide sulfonamide 13, a 78-nM JAK-2 inhibitor.
- Antonysamy, Stephen,Hirst, Gavin,Park, Frances,Sprengeler, Paul,Stappenbeck, Frank,Steensma, Ruo,Wilson, Mark,Wong, Melissa
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scheme or table
p. 279 - 282
(2009/04/16)
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- SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease
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SAR on the phenethylamide 1 (Ki 1.2μM) in the P2- and the P′-position led to potent inhibitors, one of which showed good exposure and low clearance when administered intramuscularly to rat.
- Malancona, Savina,Colarusso, Stefania,Ontoria, Jesus M.,Marchetti, Antonella,Poma, Marco,Stansfield, Ian,Laufer, Ralph,Di Marco, Annalise,Taliani, Marina,Verdirame, Maria,Gonzalez-Paz, Odalys,Matassa, Victor G.,Narjes, Frank
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p. 4575 - 4579
(2007/10/03)
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- Processes for the preparation of 2,3-dihydrothiepine derivatives
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A process for preparing a compound represented by the following formula: wherein each symbol is as defined below, or a salt thereof, characterized by subjecting a compound represented by the following formula: wherein R1 is an electron-attracting group; R2, R3, R4, R5, R6 and R7 are each a hydrogen atom, a halogen atom, an optionally substituted amino group, an optionally substituted hydroxyl group, an optionally substituted thiol group, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group, provided that R6 and R7 may be united to form a ring; and R8 is a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, to a ring-closing reaction.
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- 3,4-dihydro-4-oxo-3-(2-propenyl)-1-phthalazineacetic acids and derivatives, their preparations and medicines containing them
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Novel 3,4-dihydro-4-oxo-3(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) STR1 in which R1 R2 and R3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R4 residue such as defined below, except when R4 is H; R4 and R5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R4 and R5 do not simultaneously denote H; R6 stands for hydroxy or alkoxy radical; R7 stands for H, a halogen, a linear or branched aliphatic saturated or unsaturated radical, an alkoxy radical, said radicals being substituted or not by analiphatic or halogenated radical, a nitro group, a substituted or unsubstituted amino group, S(O)n R8 or a cyano group; n is equal to 0,1 or 2; R8 is an aliphatic, linear or branched radical, an aryl or heteroaryl radical, an amino radical, said radicals being substituted or not by an aliphatic or halogenated radical. This invention also relates to the optional tautomeric forms of said acids and their pharmaceutically acceptable base addition salts. Also described is a process for preparing said compounds and the drugs containing same.
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