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Letters in Organic Chemistry


ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Thienopyridone Antibacterials. Part IV[1]. Synthesis of Some N(7)- Heteroaryl-4-oxothieno[2,3-b]pyridine-5-carboxylic Acids and Esters

Author(s): Nuha I. Sweidan, Musa Z. Nazer, Mustafa M. El-Abadelah and Wolfgang Voelter

Volume 7, Issue 1, 2010

Page: [79 - 84] Pages: 6

DOI: 10.2174/157017810790533977

Price: $65


A series of 7-heteroaryl-4-oxo-4,7-dihydrothieno[2,3-b]-pyridine-5-carboxylic acids (8a-d) and their methyl esters (7a-d) were prepared by cyclization of the respective 2-(2,5-dichlorothien-3-yl)-3-(N-heteroarylamino)acrylates (6a-d). The latter are accessible from methyl 2-(2,5-dichlorothien-3-yl)-3-ethoxyacrylate (5) which is obtained via methyl 3-(2,5-dichlorothien-3-yl)-3-oxopropanoate(4). Of the present series, the 7-(2-thienyl) derivative (8a) exhibited good activity, especially against E. coli and Kl. pneumoniae (MIC = 2 μg / mL).

Keywords: Enaminones, aminoazoles, regioselective cyclization, 4-oxothieno[2,3-b]pyridines, antibacterial activity

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