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This chapter reports on the reactivity, synthetic methods and uses, and biological applications of isothiazoles that have been developed in the decade 1996–2006.Particular attention has been paid to the new aspects of both theoretical and experimental methods. The reactivity of conjugated rings, nonconjugated rings, and substituents attached to the rings is considered, especially original and innovative reactions.The methods presently available for the synthesis of the isothiazole ring are also treated. A variety of strategies have been developed in the last decade for the synthesis of the isothiazole ring system and new applications of well-known routes have also been described. Most of the methodologies reviewed are based on the cyclization of key intermediates through the formation of one bond. Several procedures based on the formation of two bonds are also presented. A section of the chapter is dedicated to the principal methods based on the transformation of other heterocycles into isothiazoles. Considering the broad range of useful properties manifested by various representatives of this class of compounds, a section is dedicated to their chemical, industrial, and biological applications.

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