| 摘要 |
Imidazo-[2,1-b] thiazole derivatives of the formula <FORM:1109149/C2/1> (wherein the 2,3-bond is a single or double bond and Ar is thienyl, furyl, naphthyl, benzyl or phenyl optionally halo, nitro, amino or trifluoromethyl substituted, but excluding the 2,3-unsaturated 5-benzyl compound) and acid-addition salts thereof are prepared by ring closure of an acid-addition salt of a base of the formula <FORM:1109149/C2/2> and an aromatic sulphonic acid, which itself may be prepared from the appropriate Ar-substituted ethylene oxide and 2-amino-2-thiazoline or 2-amino-thiazole in a C1- 10 alkanol followed by addition of the required aromatic sulphonic acid. The ring closure may be effected with a cyclization agent such as sulphuric or polyphosphoric acid or by conversion of the hydroxy compound to the corresponding halogeno compound (by reaction, for example, with a phosphorus halide or oxyhalide or thionyl chloride) which may or may not be isolated, and cyclization of this with a base.
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