- Metal-free oxidative: Para -acylation of unprotected anilines with N-heteroarylmethanes
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A selective oxidative para-acylation of unprotected anilines with methyl groups in N-heteroarylmethanes was achieved. This transformation proceeds under mild metal-free reaction conditions to produce the corresponding valuable diarylmethanones in good to high yields, featuring high site-selectivity, high functional-group-tolerance, gram-scale synthesis and easy product-derivation. Preliminary mechanistic studies revealed that the present oxidative para-acylation would take place via a Friedel-Crafts-type process of in situ imines and the steric hindrance might be the key issue for the high regio-selectivity.
- Liu, Min,Chen, Xue,Chen, Tieqiao,Xu, Qing,Yin, Shuang-Feng
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supporting information
p. 9845 - 9854
(2017/12/08)
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- Base metal-catalyzed benzylic oxidation of (aryl)(heteroaryl)methanes with molecular oxygen
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The methylene group of various substituted 2- and 4-benzylpyridines, benzyldiazines and benzyl(iso)quinolines was successfully oxidized to the corresponding benzylic ketones using a copper or iron catalyst and molecular oxygen as the stoichiometric oxidant. Application of the protocol in API synthesis is exemplified by the alternative synthesis of a precursor to the antimalarial drug Mefloquine. The oxidation method can also be used to prepare metabolites of APIs which is illustrated for the natural product papaverine. ICP-MS analysis of the purified reaction products revealed that the base metal impurity was well below the regulatory limit.
- Sterckx, Hans,De Houwer, Johan,Mensch, Carl,Herrebout, Wouter,Tehrani, Kourosch Abbaspour,Maes, Bert U.W.
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supporting information
p. 144 - 153
(2016/04/05)
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- Urea thiadiazole inhibitors of plasminogen activator inhibior-1
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Methods of treating disorders associated with elevated levels of PAI-1 are disclosed comprising administering to a patient in need thereof a therapeutically effective amount of at least one compound of formula (I), or a pharmaceutically-acceptable salt, prodrug, stereoisomer or solvate thereof, wherein: A is aryl o heteroaryl, and R1-R12, are defined herein. The invention also pertains to pharmaceutical compositions and compounds within the scope of formula (I) as well as medicaments and articles of manufacture comprising compounds of formula (I).
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Page/Page column 20
(2010/02/11)
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- Studies on the Insecticidal Activities of Some New N-Benzoyl-N'-Arylureas
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This paper reports the synthesis and the insecticidal activities of some N-benzoyl-N'-arylureas 4-arylsubstituted with alkylated or halogenated aroyl moieties. The compounds, tested against some representative insect species, displayed very high activity against Aedes aegypti, especially the halosubstituted derivatives. None of the newly synthesized compounds showed genotoxic activity in the Bacillus subtilis rec-assay and in the Salmonella-microsome test.
- Carmellino, Maria L.,Pagani, Giuseppe,Pregnolato, Massimo,Terreni, Marco,Caprioli, Vincenzo,Zani, Franca
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p. 227 - 236
(2007/10/03)
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