The well-decorated arylated benzo[b]thiophene scaffold is a pivotal structural motif with diverse applications in medicinal chemistry. This paper outlines a de novo synthesis of C3-arylated benzo[b]thiophenes, showcasing its flexibility and efficiency. The methodology involves Pd-catalyzed coupling of N-tosylhydrazones with (2-bromophenyl)(methyl)sulfane derivatives, followed by cyclization under mild conditions using [bis-(trifluoroacetoxy)iodo]benzene (PIFA) to yield the desired C3-arylated benzo[b]thiophenes. Substrate scope investigations and a gram-scale reaction underscore this protocol's synthetic potential and scalability. The developed approach offers a concise and versatile strategy for accessing this important class of compounds, providing a valuable tool for medicinal chemistry and pharmaceutical research.

中文翻译：

---

PIFA 介导的甲基（2-（1-苯基）苯基）硫烷环化，用于 C3-芳基苯并[b]噻吩的简洁、灵活且可扩展的从头合成


装饰精美的芳基苯并[b]噻吩支架是一个关键的结构基序，在药物化学中有多种应用。本文概述了 C3-芳基苯并[b]噻吩的从头合成，展示了其灵活性和效率。该方法包括 N-甲苯腙与（2-溴苯基）（甲基）硫烷衍生物的 Pd 催化偶联，然后在温和条件下使用 [双-（三氟乙酰氧基）碘]苯 （PIFA） 进行环化，以产生所需的 C3-芳基苯并[b]噻吩。底物范围研究和克级反应强调了该方案的合成潜力和可扩展性。开发的方法为获取这类重要的化合物提供了一种简洁而通用的策略，为药物化学和药物研究提供了有价值的工具。