Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
One-pot expedient and direct carbamoylation of heterocyclics is described. The transformation is realized via direct dehydrogenative aminocarbonylation of heterocyclic compounds under transition-metal-free conditions. This method is regioselective and the protocol is proved to be scalable on a gram scale. Further, the therapeutically useful antitubercular agent pyrazinecarboxamide is successfully synthesized by employing this protocol.
Mete, Trimbak B.,Singh, Ankit,Bhat, Ramakrishna G.
supporting information
p. 4709 - 4712
(2017/11/21)
Manganese oxide promoted liquid-phase aerobic oxidative amidation of methylarenes to monoamides using ammonia surrogates
In the presence of amorphous MnO2, various methylarenes (even with two or more methyl groups) could be selectively converted into the corresponding primary monoamides in moderate to high yields. The observed catalysis was truly heterogeneous, and the retrieved amorphous MnO2 catalyst could be reused without an appreciable loss of its catalytic performance. Copyright
Wang, Ye,Yamaguchi, Kazuya,Mizuno, Noritaka
supporting information; experimental part
p. 7250 - 7253
(2012/08/28)
1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation
A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: STR1 wherein R1 -R6 are as described in the specification; or a pharmaceutically-acceptable salt thereof.
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(2008/06/13)
Photochemical Alkylation, Hydroxyalkylation, and Alkoxylation of Pyridinecarboxamides in Alcohol
The UV-irradiation of 2- and 4-pyridinecarboxamides in alcohol brings about alkylation and/or hydroxyalkylation in the pyridine ring.In the irradiation of 3-pyridinecarboxamide in the presence of sulfuric acid, ionic reaction (alkoxylation at the 2- and 6-position) and radical reaction (alkylation at the 4- and 6-position) occur in parallel.The effects of quenchers indicate that two alkylation products originate from one excited triplet state which is quenched by energy-transfer mechanism and that two alkoxylation products originate from the excited singlet state.