- A Practical Method for Continuous Production of sp3-Rich Compounds from (Hetero)Aryl Halides and Redox-Active Esters
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A practically useful coupling reaction between aromatic halides and redox-active esters was realized by nickel catalysis through the use of a packed zinc bed column in continuous flow. Multiple reuse of the column showed a negligible decrease in efficiency, affording high space/time yields. A wide range of substrates, including a number of heteroaryl halides and polyfunctional materials were coupled in generally good yields. Longer-time and larger-scale experiments further demonstrates the robustness of the system.
- Watanabe, Eiichi,Chen, Yiding,May, Oliver,Ley, Steven V.
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supporting information
p. 186 - 191
(2019/12/24)
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- SUBSTITUTED BICYCLE HETEROCYCLIC DERIVATIVES USEFUL AS ROMK CHANNEL INHIBITORS
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Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is (II) or (III); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3, L1, L2, R1a, R1b, R1c, and n are define herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
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Page/Page column 45; 46
(2018/06/06)
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- An accessible bicyclic architecture for synthetic lectins
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Bicyclic carbohydrate receptors are easier to synthesise than tri- or tetra-cyclic relatives, and are better adapted to bind monosaccharide residues with bulky appendages. Disaccharides containing β-glucosyl units are preferred substrates.
- Howgego, Joshua D.,Butts, Craig P.,Crump, Matthew P.,Davis, Anthony P.
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supporting information
p. 3110 - 3112
(2013/06/27)
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- SUBSTITUTED DIHYDROPYRAZOLONES FOR TREATING CARDIOVASCULAR AND HEMATOLOGICAL DISEASES
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The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.
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Page/Page column 19-20
(2010/12/29)
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- THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS
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The invention provides compounds of formula I [INSERT CHEMICAL STRUCTURE HERE] (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
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Page/Page column 15
(2010/03/31)
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- THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS
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The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease
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Page/Page column 46-47
(2008/12/04)
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- Pyridobenzazepine compounds and methods for inhibiting mitotic progression
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This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treat
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Page/Page column 42-43
(2008/06/13)
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- 6-ARYLALKYLAMINO- 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS
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The present invention provides 6-substituted 2,3,4,5-tetrahydro-lH- benzo[d]azepines of Formula (I) as selective 5-HT2c receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety, where, R6 is -NR10R11, where R10 is substituted phenylalkyl or substituted pyridylalkyl and other substituents are as defined in the specification.
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Page/Page column 85-86
(2010/11/26)
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- A generic approach for the catalytic reduction of nitriles
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The scope of nickel boride mediated reduction of nitriles has been extended further to allow the preparation of Boc protected amines via a mild catalytic process. It is noteworthy that the toxicity of this procedure is greatly reduced due to its catalytic
- Caddick, Stephen,Judd, Duncan B.,Lewis, Alexandra K. De K.,Reich, Melanie T.,Williams, Meredith R. V.
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p. 5417 - 5423
(2007/10/03)
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- Convenient synthesis of protected primary amines form nitriles
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Investigations into the use of nickel chloride and sodium borohydride for the reduction of nitriles showed the secondary amine dimers to be the major products under normal conditions. The addition of a suitable trapping agent, such as di-tert-butyl dicarbonate, allowed the isolation of the protected primary amines. (C) 2000 Elsevier Science Ltd.
- Caddick, Stephen,De K. Haynes, Alexandra K.,Judd, Duncan B.,Williams, Meredith R.V.
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p. 3513 - 3516
(2007/10/03)
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