- Methanetricarboxylates as key reagents for the simple preparation of heteroarylcarboxamides with potential biological activity. Part 2 [1]. Reaction of methanetricarboxylates with 2-aminopyridine, 2-aminopyrimidine, 2-aminothiazole and 2-aminobenzothiazole
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The reaction of methanetricarboxylates 1a,b with 2-aminopyridine, 2- aminopyrimidine, 2-aminothiazole as well as 2-aminobenzothiazole yields corresponding heteroarylcarboxylic acid esters 2a,b, 5, 8, 11a,b. These heterocyclic esters were used as a starting material by the reaction with primary amines to obtaining a number of heteroarylcarboxylic amides 4a-j, 6, 10a,b, 13a-g bearing various substituents on the carboxamide group.
- Kutyrev, Alexander,Kappe, Thomas
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p. 237 - 240
(2007/10/03)
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- The Chemistry of 5-Oxodihydroisoxazoles. XIV. Synthesis of 2-(1-Aryltetrazol-5-yl)propanoic Acids
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A number of N-arylisoxazol-5(2H)-ones (aryl = phenyl, isoquinolin-1-yl, quinolin-2-yl, 2-phenylquinazolin-4-yl and benzothiazol-2-yl) have been reacted with lithium azide to give 2-(1-aryltetrazol-5-yl)acetic esters, which have been C-methylated and hydrolysed.The resulting 2-(1-aryltetrazol-5-yl)propanoic acid had low antiinflammatory activity, as judged by inhibition of synthesis of prostaglandin PGE2 or tumor necrosis factor α.
- Caiazza, Daniela,Prager, Rolf H.,Schafer, Karl
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p. 1861 - 1872
(2007/10/03)
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- Base-Catalysed Rearrangement of Isoxazolinyl Heterocycles: Synthesis of Annelated Pyrimidines
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The rearrangement of a number of ethyl 2-(heterocyclic)-5-oxo-2,5-dihydroisoxazole-4-carboxylates by mild base is described, leading to new syntheses of the pyrimidoisoquinoline, pyrimidoquinoline, pyrimidobenzothiazole, pyrimido1,2-
- Donati, Cosimo,Janowski, Wit K.,Prager, Rolf H.,Taylor, Max R.,Vilkins, Louise M.
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p. 2161 - 2169
(2007/10/02)
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