A variety of dyes, agrochemicals, and natural products often use a 2-aminothiophene component in its skeletal backbone. 2-Aminothiophene derivatives exhibit a diverse set of therapeutic activities such as anti-inflammatory, anti-convulsant, and anti-microbial activities. Some marketed drugs such as olanzapine and clotiazepam were developed upon a 2-aminothiophene scaffold. Due to thier significant advantages, more recently, there is a growing interest in research for the efficient and convenient synthesis of 2-aminothiophenes. In this contribution, a simple and efficient continuous-flow procedure for the synthesis of substituted 2-aminothiophenes under continuous-flow conditions using the spinning tube-in-tube (STT�) has been described (Scheme 1). The scope of the reaction involves a a-methylene carbonyl compound reacted with and activated methylene substrate. This protocol demonstrates high exploratory power, and atom efficiency for establishing the assembly of a variety of functionalized 2-aminothiophene scaffolds in high yields.

Multicomponent flow approach for the efficient and more sustainable preparation of aminothiazole derivatives

248th National Meeting (2014)

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