A concise total synthesis of (-)-quinocarcin via aryne annulation.

One-pot synthesis of 1-alkyl-1H-indazoles from 1,1-dialkylhydrazones via aryne annulation.

The reaction of readily accessible 1,1-dialkylhydrazones with commercially available o-(trimethylsilyl)aryl triflates provides a direct one-step route to pharmaceutically important 1-alkylindazoles. The products are obtained in high yields by one-pot NCS-chlorination/aryne annulation or Ac(2)O-acylation/deprotection/aromatization protocols.

Orthogonal synthesis of indolines and isoquinolines via aryne annulation.

Concise Enantiospecific Total Synthesis of Tubingensin A

We report the enantiospecific total synthesis of (+)-tubingensin A. Our synthesis features an aryne cyclization to efficiently introduce the vicinal quaternary stereocenters of the natural product and proceeds in only nine steps (longest linear sequence) from known compounds.

Synthesis of Poly-Substituted Quinolines via Friedländer Hetero-Annulation Reaction Using Silica-Supported P2O5 under Solvent-Free Conditions

A highly efficient, simple and green solvent-free protocol for the preparation of poly-substituted quinolines via Friedländer hetero-annulation reaction between 2-aminoaryl ketones and carbonyl compounds in the presence of silica-supported P2O5 (P2O5 / SiO2) is described. In this method, the title compounds are obtained in high to exc...

Cascade annulation of malonic diamides: a concise synthesis of polycyclic pyrroloindolines.

A concise synthesis of polycyclic pyrroloindolines from simple malonic diamides via an intramolecular oxidative coupling/condensative cyclization cascade process is reported. The reaction provides an efficient method to construct polycyclic pyrroloindolines in good to excellent yields, which should be useful in the synthesis of natural products and pharmaceutical molecules.