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Transition-Metal-Free Synthesis of <i>N-</i>Arylphenothiazines through an <i>N</i>- and <i>S</i>-Arylation Sequence

Tsubasa Matsuzawa, Takamitsu Hosoya, Suguru Yoshida

2021Organic Letters27 citationsDOI

Abstract

An efficient synthetic method of N-arylphenothiazines from o-sulfanylanilines under transition-metal-free conditions is disclosed. An N- and S-arylation sequence of o-sulfanylanilines enabled us to synthesize a wide variety of N-arylphenothiazines. In particular, one-pot synthesis of N-arylphenothiazines was accomplished from easily available modules through preparation of o-sulfanylanilines by thioamination of aryne intermediates and following N- and S-arylation sequence.

Topics & Concepts

ChemistrySequence (biology)AryneTransition metalStereochemistryCombinatorial chemistryMetalMedicinal chemistryOrganic chemistryCatalysisBiochemistryPhenothiazines and Benzothiazines Synthesis and ActivitiesSulfur-Based Synthesis TechniquesSynthesis and Catalytic Reactions
Transition-Metal-Free Synthesis of <i>N-</i>Arylphenothiazines through an <i>N</i>- and <i>S</i>-Arylation Sequence | Litcius