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Synthesis of 4-(Isothiazol-3-yl)morpholines and 1-(Isothiazol-3-yl)piperazines, and Their Inhibitory Activity towards Acetylcholinesterase

✍ Scribed by Janine Wolf; Camino M. González Tanarro; Michael Gütschow; Joachim Sieler; Bärbel Schulze


Publisher
John Wiley and Sons
Year
2008
Tongue
German
Weight
273 KB
Volume
91
Category
Article
ISSN
0018-019X

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✦ Synopsis


Abstract

The synthesis of novel triaryl‐substituted 4‐(isothiazol‐3‐yl)morpholines 7 and 8, and 1‐(isothiazol‐3‐yl)piperazines 913 by reaction of the corresponding isothiazolium salts 5 and 6 with secondary amines in the presence of t‐BuOK in absolute THF is described. Some representatives of the isothiazoles were evaluated as inhibitors of acetylcholinesterase from Electrophorus electricus.


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## Abstract A series of novel 1‐[(1__R__)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethyl]‐3‐substituted phenyl ureas were synthesized by the condensation of (1__R__)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethanamine with substituted phenyl isocyanates under mild conditions. Their structures were confirmed ^1^H