A convenient synthesis of 2-acyl benzothiazoles/thiazoles from benzothiazole/thiazole and N,N'-carbonyldiimidazole activated carboxylic acids |
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| Authors: | Tonghui Huang Xin Wu Yongbo Yu Lin An Xiaoxing Yin |
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| Institution: | 1. Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, Jiangsu 221000, PR China;2. Xuzhou Medical University Science Park, Xuzhou, Jiangsu 221006, PR China |
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| Abstract: | A convenient and efficient strategy for the synthesis of 2-acyl benzothiazoles/thiazoles has been developed. The treatment of benzothiazole/thiazole with allylic Grignard reagents readily generates the corresponding 2-Grignard reagents, which is followed by a reaction with N,N'-carbonyldiimidazole activated carboxylic acids to afford various 2-acyl benzothiazoles/thiazoles products. The synthetic method is applicable to a wide array of carboxylic acids and allows easy access to 2-acyl benzothiazoles/thiazoles with considerable yields under mild reaction conditions. |
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| Keywords: | Corresponding author 2-Acyl thiazoles 2-Acyl benzothiazoles Grignard reagents Acylation |
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