A convenient method for the synthesis of 2-amino substituted aza-heterocycles from N,N′-disubstituted thioureas using TsCl/NaOH
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
A mild cyclodesulfurization of N-(2-hydroxyethyl)-N′-phenylthioureas to 2-phenylamino-2-oxazolines using TsCl/NaOH
An efficient synthesis of 2-phenylamino-2-oxazolines 3 via cyclodesulfurization of N-(2-hydroxyethyl)-N′-phenylthioureas 2 by a one-pot reaction using p-toluenesulfonyl chloride (TsCl) and NaOH in very good yields is described.
Kim, Taek Hyeon,Lee, Namgun,Lee, Gue-Jae,Kim, Jae Nyoung
p. 7137 - 7141
(2007/10/03)
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