5093-70-9Relevant articles and documents
A 2, 6 - dimethyl -4 - bromo pyridine synthesis method
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Paragraph 0011; 0014-0015; 0018-0020; 0022, (2019/05/28)
The invention relates to the field of organic chemistry, in particular to a 2, 6 - dimethyl - 4 - bromo pyridine synthesis method, comprises the following steps: malonic acid diethyl ester and alkali metal reaction to produce salt, then dropwise 4 - nitro - 2 - methyl - 6 chloro pyridine to a toluene solution of a condensation reaction, after decarboxylation under acidic conditions to the 4 - nitro - 2, 6 - dimethyl pyridine; 4 - nitro - 2, 6 - dimethyl pyridine in under the catalysis of the Pd/C, methanol as the solvent, hydrogen reduction, filtered, the filtrate is concentrated, from 4 - amino - 2, 6 - dimethyl pyridine; 4 - amino - 2, 6 - dimethyl pyridine first with an acid generating salt, cooled to - 15 °C - 3 °C, [...], drops the instillment sodium nitrite aqueous solution, pH adjusting solution is dropped is alkaline, and then extracted, dried, concentrated, be 2, 6 - dimethyl - 4 - bromo pyridine. The method of the invention is beneficial effect: mild reaction conditions, high yield, and raw materials are easy, and the cost is low, the process route is short, and has industrial prospects.
Meta halogenation of 1,3-disubstituted arenes via iridium-catalyzed arene borylation
Murphy, Jaclyn M.,Liao, Xuebin,Hartwig, John F.
, p. 15434 - 15435 (2008/09/19)
We report the meta halogenation of 1,3-disubstituted arenes to form 3,5-disubstituted aryl bromides and chlorides by using iridium-catalyzed arene borylation chemistry. Iridium-catalyzed borylation of arenes with B2pin2, followed by reaction of the boronic ester with copper(II) bromide or chloride converts arylboronic esters to the corresponding aryl halides. A variety of arenes containing alkoxy, alkyl, halogen, nitrile, ester, amide, and pivaloyl and TIPS-protected alcohols were converted to the corresponding 3,5-disubstituted aryl bromides and chlorides in yields ranging from 46% to 85%. In addition, 2,6-disubstituted and 3-substituted pyridines were converted to the 4-halo and 5-halopyridines, respectively. The utility of this methodology was demonstrated by the formal conversion of nicotine to Altinicline in three steps with an overall yield of 61% using meta bromination of nicotine as the first step. Copyright
ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
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Page/Page column 62-63, (2010/02/11)
The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
