65346-04-5Relevant articles and documents
Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
Mete, Trimbak B.,Singh, Ankit,Bhat, Ramakrishna G.
supporting information, p. 4709 - 4712 (2017/11/21)
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.
PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
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Page/Page column 152; 153, (2014/09/29)
PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE ABSTRACT OF THE DISCLOSURE The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: {INSERT STRUCTURE HERE} I wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
A Simple Synthesis of 5-Cyano-2-pyridinecarboxylic Acid and its Amide
Langhals, Elke,Langhals, Heinz,Ruechardt, Christoph
, p. 1259 - 1261 (2007/10/02)
The title compounds 3 and 2 (X = CN) are prepared in good yields by regioselective carbamoylation of 3-cyanopyridine in a Minisci reaction and by consecutive amide hydrolysis with amyl nitrite in HCl-saturated acetic acid.The observed regioselectivity apparently remains confined to carbamoyl and possibly acyl radicals and to -M-effect substituents in 3-position.