Abstract Die erste nicht‐dirigierte dehydrierende Kupplungsmethode zur Herstellung von Phenonen über Toluole mit aromatischen C−H Bindungen wird hier großem Substratspektrum gezeigt. Diese Reaktion zeigt eine deutlich atom‐ und schritteffizientere Alternative zu klassischen Friedel–Crafts oder Suzuki–Miyaura inspirierten Acylierungsreaktionen. Methode kann auch im Gramm‐Maßstab ausgeführt werde...

Enantiomerically enriched indolines and tetrahydroisoquinolines were synthesized within 5 min to 2 h in high yields from easily accessible (S)-amino acid derived chiral carbocations. The diastereoselective Friedel-Crafts reaction is promoted by a Lewis acid (AlCl3) offering trans-diastereoselectivity. The rate of the reaction and diastereoselectivity of the product are significantly influenced ...

A novel study of external Brønsted acid-assisted thiourea catalysts in the asymmetric FriedelCrafts alkylation of indoles with nitroalkenes is reported. The final 3-substituted indoles derivatives are synthesized with better results by cooperative effect between chiral thiourea and a Brønsted acid additive (1a·HA), than those obtained with sole thiourea catalyst 1a. The effect of diverse catal...

An efficient and practical procedure for the synthesis of esonarimod, (R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (1), a new antirheumatic drug, has been developed. The intermediate, 2-methylene-4-(4-methylphenyl)-4-oxobutanoic acid (2), was prepared by Friedel-Crafts acylation of toluene with itaconic anhydride (3) in the presence of aluminum trichloride and nitrobenzene in ...

Single-walled carbon nanotubes (SWCNTs), which were commercial grade containing 60–70 wt% impurity, were treated in a mild poly(phosphoric acid) (PPA). The purity of PPA treated SWCNTs was greatly improved with or without little damage to SWCNTs framework and stable crystalline carbon particles. An amide model compound, 4-(2,4,6-trimethylphenoxy)benzamide (TMPBA), was reacted with SWCNTs in PPA...

The first total synthesis of (+)-gliocladin B is described. Our concise and enantioselective synthesis takes advantage of a new regioselective Friedel-Crafts-based strategy to provide an efficient multigram-scale access to the C3-(3'-indolyl)hexahydropyrroloindole substructure, a molecular foundation present in a significant subset of epipolythiodiketopiperazine natural alkaloids. Our first-gen...

Total synthesis of naturally occurring spirobisnaphthalene palmarumycin CP17 and its methoxy analogues was first achieved through Friedel-Crafts acylation, Wolff-Kishner reduction, intramolecular cyclization, ketalization, benzylic oxidation, and demethylation using the inexpensive and readily available methoxybenzene, 1,2-dimethoxybenzene and 1,4-dimethoxybenzene and 1,8-dihydroxynaphthalene a...