Practical preparation of ethyl 2-methylthiophene-3-carboxylate
Masakazu Kogami1, Nobuhide Watanabe
1Drug Discovery Laboratories, Sanwa Kagaku Kenkyusho Co. Ltd., 363 Shiosaki, Hokusei-cho, Mie, Japan.
Abstract:
A safe and efficient process for the preparation of ethyl 2-methylthiophene-3-carboxylate (5) was devised. This process provides several advantages over the precedents, involving operational simplicity, avoidance of the use of strong bases such as n-butyllithium and application of noncryogenic conditions, and enabled to prepare 5 in 52% overall yield from commercially available 2-methylthiophene on a multikilogram scale.
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