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Elemental-Sulfur-Incorporated Cyclizations of Pyrrolidines Leading to Thienopyrroles

Yuanyuan Yue, Huibin Shao, Zhixian Wang, Ke Wang, Le Wang, Kelei Zhuo, Jianming Liu

2020The Journal of Organic Chemistry14 citationsDOI

Abstract

We report, herein, the synthesis of thieno[3,2-b]pyrroles from the direct oxidative [4 + 1] cyclization of 2-alkynyl pyrrolidines with elemental sulfur. This transformation likely originates from electrophilic attack at the β-position of pyrrolidine followed by an intramolecular thienannulation to deliver the desired product. Mechanistic investigation suggests that the present reaction involves the formation of dihydrothieno[3,2-b]pyrrole as an intermediate.

Topics & Concepts

ChemistryPyrrolidineSulfurIntramolecular forceElectrophilePyrroleElemental analysisCombinatorial chemistryOxidative phosphorylationMedicinal chemistryOrganic chemistryCatalysisBiochemistrySulfur-Based Synthesis TechniquesSynthesis and Characterization of PyrrolesOrganic Chemistry Cycloaddition Reactions
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