A chiral phosphoric acid catalyzed stereoselective Michael addition of 5H‐thiazol‐4‐ones to arylazocarboxylates was developed for the construction of optically active N,S‐acetal frameworks. Both 1‐naphthylazocarboxylates and phenylazocarboxylates were compatible to afford a series of 1,4‐adducts in generally high yields and enantioselectivities. Notably, the catalytic protocol enables the formation

A regioselective one‐pot approach to the synthesis of C4‐alkylated tetrahydropyridines (THPs) and tetrahydroquinolines (THQs) by dearomatization of pyridines and quinolines has been developed. The transformation is achieved by the BF 3 •OEt 2 ‐mediated, C4‐selective addition of Grignard reagents, followed by a cascade of enamine protonation and the subsequent Et 3 SiH reduction of the resulting iminium

This minireview summarizes important collection of cycloaddition strategies that were used for the synthesis of sulfur‐containing five‐ and six‐membered heterocycles from thiocarbonyl‐based synthons. Among various stepwise or concerted methods available to prepare thioheterocycles, cycloaddition reactions of thiocarbonyls in particular present an important class of reaction owing to their ability to

We have developed an iron(III) chloride hexahydrate catalyzed formal [3+2] cycloaddition of tetrahydroisoquinolines with amide group‐bearing Morita‐Baylis‐Hillman (MBH) carbonates. A range of highly functionalized dihydropyrrolo[2,1‐a]isoquinolines could be prepared through SN2’/oxidation/ electrocyclization/aromatization cascade (32‐62% yield).

Near infrared (NIR)‐emissive polymers are attractive luminescent materials due to their utilities inbiological, optoelectronic, and telecommunication applications. Herein we report the use of a dialkylamine‐strapped dithienylpyrrole (DTP) as an excited‐state intramolecular proton transfer (ESIPT) building block for producing NIR‐emissive π‐conjugated polymers. The study of a series of model compounds

An organocatalytic enantioselective Michael addition of 5 H ‐thiazol‐4‐ones to 1‐azadienes has been developed. In the presence of chiral phosphoric acid, a series of optically active benzofuran derivatives featured by vicinal sulfur‐containing quaternary and tertiary stereocenters were obtained in high yields (42‐99%) with high stereoselectivities (15‐96% ee and 2:1‐>20:1 dr).

An efficient access to chiral pyrrolidine derivatives bearing one trifluoromethylated quaternary stereogenic centers is developed through Cu(I)/( S )‐TF‐BiphamPhos‐catalyzed asymmetric 1,3‐dipolar cycloaddition of azomethine ylides with tert ‐butyl 2‐(trifluoromethyl)acrylate in moderate to high yields, excellent diastereoselectivities and good enantioselectivities (up to 95% yield, >20:1 dr, 89% ee)

Primary thioamides are useful building blocks for drug and insecticide development, therefore an environmentally benign synthesis of primary thioamides is desired. This paper discloses an oxidative thiolysis for the selective transformation of nitriles into primary thioamides using elemental sulfur or thiuram in the presence of K 2 S 2 O 8 in DMF/H 2 O. This practical method enables access to a wide

Chemodivergent dehydrative nucleophilic substitutions of diarylmethanols with 1‐phenyl‐1H‐tetrazole‐5‐thiol were achieved using FeCl3 as a catalyst in MeNO2 by changing reaction temperature. It was found that sulfur nucleophilic attack occurred to afford kinetically controlled products that rearranged into thermodynamically controlled products. A variety of diarylmethanols could be applied to the reaction

A protocol for the isothiourea‐catalyzed enantioselective functionalization of pyrrolyl‐ and indolylacetic acids has been developed. Stereodefined dihydropyridinones are accessed through formal [4+2] cycloaddition of an in situ generated isothiouronium enolate with α,β‐unsaturated ketimines. The dihydropyridinones are obtained in moderate to excellent yield (26–97%), excellent diastereocontrol (all

Smallest ring size, high ring strain, and more reactivity of cyclopropene have brought the attention of researchers for chemical exploration. In this context, the chemistry of cyclopropene and cyclopropenone has exponentially grown over the last few years. This present review focuses on the most recent developments in cyclopropane chemistry.

Karlotoxin 2 (KmTx2) is a marine natural product isolated from the dinoflagellate Karlodinium veneficum . The absolute configuration of KmTx2 was determined by NMR analysis in combination with degradation of the natural product, and the absolute configuration at C49 was revised by computational analysis. On the other hand, we reported revision of the absolute configuration of amphidinol 3 (AM3), whose