- PROCESS FOR THE CATALYTIC DIRECTED CLEAVAGE OF AMIDE-CONTAINING COMPOUNDS
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The present invention relates to a catalytic method for the conversion of amide-containing compouds by means of a build-in directing group and upon the action of a heteronucleophilic compound (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or a thiol (RSH)) in the presence of a metal catalyst to respectively esters, thioesters, carbonates, thiocarbonates and to what is defined as amide-containing compounds (such as carboxamides, urea, carbamates, thiocarbamates). The present invention also relates to these amide-containing compounds having a build-in directing group (DG), as well as the use of such directing groups in the catalytic directed cleavage of N-DG amides with the use of heteronucleophiles (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or thiol (RSH)).
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Page/Page column 51; 54
(2017/04/11)
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- Aminoquinazolines as TRPV1 antagonists: Modulation of drug-like properties through the exploration of 2-position substitution
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A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflammator
- Blum, Charles A.,Zheng, Xiaozhang,Brielmann, Harry,Hodgetts, Kevin J.,Bakthavatchalam, Rajagopal,Chandrasekhar, Jayaraman,Krause, James E.,Cortright, Daniel,Matson, David,Crandall, Marci,Ngo, Chu K.,Fung, Lawrence,Day, Marta,Kershaw, Mark,De Lombaert, Stephane,Chenard, Bertrand L.
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body text
p. 4573 - 4577
(2009/04/06)
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- SOME NEW 2-SUBSTITUTED 5-TRIFLUOROMETHYLPYRIDINES
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The preparation of the derivatives of 2-amino-, hydrazino-, hydroxy-, and mercapto-5-trifluoromethylpyridines via 2-chloro precursors is describes.Experimental and spectral data of the products together with those of the precursors are presented.
- Haga, Takahiro,Fujikawa, Kan-ichi,Koyanagi, Tohru,Nakajima, Toshio,Hayashi, Kouji
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p. 117 - 124
(2007/10/02)
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