Convenient Method for the Preparation of the 2-Methyl Thiophen-3-yl Magnesium Bromide Lithium Chloride Complex and Its Application to the Synthesis of 3-Substituted 2-Methylthiophenes |
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| Authors: | Masakazu Kogami |
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| Affiliation: | Drug Discovery Laboratories , Sanwa Kagaku Kenkyusho Co., Ltd. , Mie , Japan |
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| Abstract: | Lithium chloride was found to accelerate formation of the Grignard reagent from inactive 3-bromo-2-methylthiophene (1) and commercial magnesium metal. Based on this finding, a convenient and potentially scalable preparation of ethyl 2-methylthiophene-3-carboxylate (3) was achieved. In addition, this process has been found to provide a new, general approach to 3-substituted 2-methylthiophenes. |
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| Keywords: | Activator 3-bromo-2-methylthiophene Grignard reagent lithium chloride |
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