65295-68-3Relevant academic research and scientific papers
A convenient method for the synthesis of 2-amino substituted aza-heterocycles from N,N′-disubstituted thioureas using TsCl/NaOH
Heinelt, Uwe,Schultheis, Daniela,J?ger, Siegfried,Lindenmaier, Marion,Pollex, Annett,Beckmann, Henning S.G.
, p. 9883 - 9888 (2007/10/03)
p-Toluenesulfonyl chloride (TsCl)/NaOH has been introduced as reagent combination for the synthesis of 2-amino-oxa- or 2-amino-thiazolidines from N-(2-hydroxyethyl)-thioureas, but its general application in heterocycle synthesis has not been investigated. In this paper the convenient and efficient synthesis of a variety of 2-amino-substituted 1-aza 3-(aza, oxo or thio) heterocycles of different substitution and ring sizes is described. The application of polymer-supported TsCl facilitates work-up and renders the reaction conditions very suitable for parallel or robot synthesis. Graphical Abstract
Process for synthesizing heterocyclic compounds
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Page/Page column 13, (2008/06/13)
The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine of formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.
Antihypertensive (2-Aminoethyl)thiourea Derivatives. 1
Tilley. Jefferson W.,Levitan, Paul,Kierstead, Richard W.,Cohen, Michael
, p. 1387 - 1392 (2007/10/02)
Structure-activity studies were carried out on a series of antihypertensive 1-(2-aminoethyl)-3-(substituted phenyl)thioureas.From this class of compounds, the 2,6-dichlorophenyl analogue 2 was found to have potent oral antihypertensive activity in two hypertensive rat models and the renal hypertensive dog.In addition to its effect on blood pressure, 2 displayed sedative effects which had a marked species specificity.
Thiourea derivatives
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, (2008/06/13)
Antihypertensively active thiourea derivatives of the formulas STR1 wherein R, R1, R2, R3 and X are as hereinafter described, as well as a method of using a compound of the formula STR2 wherein R1 ', R2 ', R3 and X are as previously described, or a compound of formula II as an anti-hypertensive agent, is described.
