- Cobalt-Catalyzed Electrophilic Amination of Aryl- and Heteroarylzinc Pivalates with N-Hydroxylamine Benzoates
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Aryl- and heteroarylzinc pivalates can be aminated with O-benzoylhydroxylamines at 25 °C within 2–4 h in the presence of 2.5–5.0 % CoCl2?2 LiCl to furnish the corresponding tertiary arylated or heteroarylated amines in good yields. This electrophilic amination also provides access to diarylamines and aryl(heteroaryl)amines. A new tuberculosis drug candidate (Q203) was prepared in six steps and 56 % overall yield by using this cobalt-catalyzed amination as the key step.
- Chen, Yi-Hung,Gra?l, Simon,Knochel, Paul
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supporting information
p. 1108 - 1111
(2018/01/01)
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- Nickel-Catalyzed Cross-Coupling of Functionalized Organo manganese Reagents with Aryl and Heteroaryl Halides Promoted by 4-Fluorostyrene
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A catalytic system consisting of Ni(acac) 2 (5 mol%) and 4-fluorostyrene (20 mol%) allows a convenient cross-coupling of functionalized organomanganese reagents with a variety of aryl and heteroaryl halides leading to polyfunctionalized diaryl- and arylheteroarylmethane derivatives.
- Benischke, Andreas D.,Desaintjean, Alexandre,Juli, Thomas,Cahiez, Gérard,Knochel, Paul
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supporting information
p. 5396 - 5412
(2017/12/14)
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- C-ARYL GLUCOSIDE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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C-aryl glucoside derivatives, preparation processes and pharmaceutical uses thereof are disclosed. In particular, C-aryl glucoside derivatives represented by formula (I), with each substituent defined in the application, pharmaceutically acceptable salts or stereoisomers thereof, their preparation methods, and pharmaceutical compositions containing the derivatives as well as their uses as therapeutic agents, particularly as sodium-dependent glucose cotransporter (SGLT)-1 inhibitors, are disclosed.
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Paragraph 0151
(2013/06/04)
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- Novel chromogenic substances and use thereof for the determination of carboxypeptidase activities
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The invention relates to chromogenic compounds and the use thereof for the determination of enzymes of the family of carboxypeptidases N and carboxypeptidases U. The above is more specifically a compound of formula (I) in which A=(1), (2), (3), (4) or (5). R1. R2=H. —CH3, —CH(CH3)2, —OCH3, —Cl.—CF3,—OCF3,—SCH3, R3=an amino acid group which may be hydrolysed by a carboxypeptidase A and R4=a basic amino acid group.
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Page/Page column 27
(2008/06/13)
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