5025-82-1Relevant articles and documents
PROCESS FOR OBTAINING MIXTURES OF 4-CARBOXY-1,3-THIAZOLIDINIUM CARBOXYLATE AND N-ACYL-1,3-THIAZOLIDIN-4-CARBOXYLIC ACID
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Page/Page column 8-9; 10, (2009/06/27)
The present invention relates to a process for obtaining in a single synthesis stage mixtures of 4-carboxy-1,3-thiazolidium carboxylate and N-acyl-1, 3-thiazolidin-4- carboxylic acids from 1,3-thiazolidin-4-carboxylic acids and derivatives of carboxylic acids, which has the following advantages: use of environmentally friendly solvents, lower energy consumption, lower consumption of acylating reagents, which allows the corresponding mixtures to be obtained with suitable characteristics and specifications, ease of recovery from the reaction medium and high yields.
Synthesis, Chemical Reactivity, and Antileukemic Activity of 5-Substituted 6,7-Bis(hydroxymethyl)pyrrolothiazole Biscarbamates and the Corresponding Sulfoxides and Sulfones
Anderson, Wayne K.,Mach, Robert H.
, p. 2109 - 2115 (2007/10/02)
A series of bis(N-methylcarbamate) and bis derivatives of 5-substituted 6,7-bis(hydroxymethyl)pyrrolothiazoles was prepared.The compounds were tested for activity in vivo against P388 lymphocytic leukemia, and the chemical reactivities of the compounds were compared by using the model nucleophile 4-(4-nitrobenzyl)pyridine (NBP).The 5-(3,4-dichlorophenyl)-substituted biscarbamates 6b, 8b, and 12b were inactive and unreactive toward NBP.The 5-methyl-substituted bicarbamates 6a, 7a, 8a, 9a, 12a, and 13a were all active against murine P388 lymphocytic leukemia.The chemical reactivities of the active compounds depended on the oxidation state of the sulfur.The reactivity toward NBP followed the order S > SO >> SO2.The sulfones 12a and 13a are the most active compounds in this series, and their lack of reactivity toward NBP led to the suggestion that 12a and 13a are activated in vivo.