112204-58-7Relevant academic research and scientific papers
C-H activation/borylation/oxidation: A one-pot unified route to meta-substituted phenols bearing ortho-/para-directing groups
Maleczka Jr., Robert E.,Shi, Feng,Holmes, Daniel,Smith III, Milton R.
, p. 7792 - 7793 (2003)
An efficient one-pot C-H activation/borylation/oxidation protocol for the preparation of phenols is described. This method is particularly attractive for the generation of meta-substituted phenols bearing ortho-/para-directing groups, as such substrates are difficult to access by other phenol syntheses. Copyright
Selective C-H bond fluorination of phenols with a removable directing group: Late-stage fluorination of 2-phenoxyl nicotinate derivatives
Lou, Shao-Jie,Chen, Qi,Wang, Yi-Feng,Xu, Dan-Qian,Du, Xiao-Hua,He, Jiang-Qi,Mao, Yang-Jie,Xu, Zhen-Yuan
, p. 2846 - 2849 (2015/05/20)
A facile and site-selective C-H bond fluorination of phenols using removable 2-pyridyloxy group as an auxiliary was developed. Alternatively, late-stage C-H bond fluorination of bioactive 2-phenoxyl nicotinate derivatives and diflufenican were also feasible under the present strategy.
BENZAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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Page/Page column 27, (2010/09/17)
The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
Preparation of monofluorophenols via the reaction of difluorobenzene derivatives with potassium trimethylsilanoate
Li, Jianqing,Smith, Daniel,Qiao, Jennifer X.,Huang, Stella,Krishnananthan, Subramaniam,Wong, Henry S.,Salvati, Mark E.,Balasubramanian, Balu N.,Chen, Bang-Chi
scheme or table, p. 633 - 637 (2009/07/01)
An efficient synthesis of monofluorophenols via the reaction of difluorobenzene derivatives with potassium trimethylsilanoate in moderate to excellent yields is described. High regioselectivity was observed in some cases. Georg Thieme Verlag Stuttgart.
TRIAZOLOANILINOPYRIMIDINE DERIVATIVES FOR USE AS ANTIVIRAL AGENTS
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Page/Page column 29, (2010/11/28)
A quinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof: formula (I) for use in treatment of prevention of a flaviviridae infection.
Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
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Page/Page column 68, (2010/11/25)
The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
PHENYLGLYCINAMIDE DERIVATIVES USEFUL AS ANTICOAGULANTS
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Page/Page column 86-87, (2008/06/13)
The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
Halogen-lithium exchange between substituted dihalobenzenes and butyllithium: Application to the regioselective synthesis of functionalized bromobenzaldehydes
Da?browski, Marek,Kubicka, Joanna,Luliński, Sergiusz,Serwatowski, Janusz
, p. 6590 - 6595 (2007/10/03)
Halogen-lithium interconversion reactions between unsymmetrically substituted mono- and bifunctional dihalobenzenes C6H 3XHal2 and C6H2XYHal2 (Hal=Br, I; X, Y=F, OR, CF3, CH(OMe)2) and butyllithium were investigated. The resultant organolithium intermediates were converted into the corresponding benzaldehydes in moderate to good yields. As a rule, bromine atoms in the position ortho to the functional group were replaced preferentially with lithium. Intramolecular competition experiments with bifunctional systems revealed that fluorine is capable of activating the neighboring bromine atom more strongly than methoxy and dimethoxymethyl groups. On the replacement of the non-activated bromine with iodine a complete reversal of this reactivity pattern can be accomplished due to the preferred iodine-lithium exchange.
MIDAZOPYRAZINONES AND IMIDAZOTRIAZINONES DERIVATES AS GABA-A RECEPTOR ANXIOLYTIC
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Page 35-36, (2008/06/13)
The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein -U-V- represents -CH=CH-, or -CH2-CH2-, -N=CH- or -CH=N-; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a -NH- or -OCH2- linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, -SO2Ra, -SO2NRaRb, -CORa, -CO2Ra or -CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group;pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.
Process for the synthesis of phenols from arenes
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Page 15; 18-21, (2008/06/13)
A process to synthesize substituted phenols such as those of the general formula RR′R″Ar(OH) wherein R, R′, and R″ are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C—H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.
