A one‐pot cascade coupling/annulation reaction for the synthesis of phenanthridines has been developed from arylboronic acids and o‐bromo arylamides with DMSO as a carbon source. The desired phenanthridines were obtained in moderate to good yields by using simple procedure.

The switchable catalytic approach for the regioselective intramolecular hydroarylation of ynone has been developed. When ZnI2 was used as catalyst, the umpolung α‐arylation of ynone was realized via an addition‐elimination process of iodine ion to generate the PQM intermediate, which could be trapped by styrene to form benzo[f,h]chromenes through hetero‐Diels‐Alder reaction. While IPrAuCl/AgSbF6 was

Indole‐containing polycyclic hetero aromatic compounds are synthesized by multistep process, which have wide application in biological activities and organic semi‐conductor materials. Here in we report the one‐pot method for the synthesis of polysubstituted indolo[2,1‐a]isoquinolines by Ru(II) catalyzed double aryl/hetero aryl C(sp2)‐H activation through in‐situ installed carbamide of phenyl isocyanate

Herein we report the first Ni(II)‐catalysed transfer hydrogenation of quinolines using ammonia borane (AB) as hydrogen (H2) source. An in situ generated Ni(II)‐bis(pyrazolyl)pyridine pre‐catalyst could hydrogenate quinoline and its derivatives in excellent yields of up to 90% at 25 °C in 30 minutes. Spectroscopic studies revealed that a Ni(II)‐hydride is responsible for the transfer hydrogenation of

A simple and efficient visible‐light‐initiated cascade reaction of 2‐isothiocyanatonaphthalenes and amines with ambient dioxygen as the sole oxidant under additive‐, external photocatalyst‐free and ambient conditions was developed. 38 Examples of N‐substituted naphtho[2,1‐d]thiazol‐2‐amines were regioselectively constructed in good to excellent yields.

Synthesis of pharmaceutically active heterocycles is always appealing as the majority of the widely used drugs contain heterocyclic moieties as their core structure. So, the straightforward construction of heterocycles from readily available/accessible reagents is one of the prime targets of the synthetic chemists. In this context, C‐H functionalization has emerged as an effective tool for the designing

A cheap and efficient C(sp3)–H phosphorylation has been achieved via the iron‐catalyzed cross‐coupling reactions between 1,3‐dicarbonyl compounds and P(O)–H compounds involving C–C bond cleavages with air as the oxidant. This transformation provides a straightforward way to construct C(sp3)–P bonds, leading to the formation of β‐ketophosphine oxides in up to 93% yield with good functional group tolerance

Phenothiazine is an important structural motif in pharmaceuticals and advanced functional organic materials. However, the C‐H functionalization reaction of N‐protected phenothiazine is rather unexplored and often shadowed by its chemical reactivity on the heteroatomic centers, which limits the diversity of its potential applications. This report demonstrates a straightforward approach towards the site‐selective

N‐(Pyrid‐2‐yl)‐substituted azolium and pyridinium salts, precursors for hybrid NHC‐containing ligands, were obtained with excellent regioselectivity, employing a deoxygenative CH‐functionalization of pyridine‐N‐oxides with substituted imidazoles, thiazoles, and pyridine. Unlike the traditional SNAr‐based methods, this approach provides high yields for substrates bearing substituents of different electronic

The importance of fluorinated organic molecules in drugs and pharmaceuticals led to the development of several synthetic methods for introducing fluorine into bioactive molecules and trifluoromethylation is one of the key approaches for the same. Electrochemical organic synthesis has emerged as one of the most sustainable, green synthetic strategies in recent years and new developments in electroorganic

While remarkable progress has recently been made for the direct C‐H‐functionalization of azines, its application is still limited by a lack of accessible functional groups (primarily carbon‐based) and poor regioselectivity. In contrast, C2‐functionalized pyridines and quinolines can be easily synthesized by treating readily available N‐oxides with various reagents under appropriate activation conditions

Molecules with di‐ or trichloromethyl group are widely existed in natural products and man‐made structures that represent special activities in pharmaceuticals and agrochemicals. Besides, polychloromethyl‐containing compounds are also high valuable intermediates in organic synthesis and also can be used as functional materials. Therefore, significant efforts have been made toward the incorporation

Indole derivatives are important heterocycles in organic synthesis for serving as privileged building blocks for functional material and as key components in a lot of bioactive compounds. Propargylic alcohols, bearing alkynyl and hydroxyl functional groups, have emerged as promising feedstock materials for the construction of carbo‐ and heterocycles. Especially, in the last decade, the Lewis or Brønsted

The trifluoromethyl (CF3) group is an advantageous structural motif in various biologically active molecules as well as materials, which is depicted by steadily increasing demand from the industries involved in drug discovery, agrochemicals and material development. β‐trifluoromethyl α,β‐unsaturated carbonyl compounds constitute a very efficient building blocks as starting material in the synthesis

Abstract: Aromatic functionalizations are of current interest and importance in organic chemistry, recent transition‐metal catalyzed reactions can transform inert C–H bond into C–X (X = C, O, N, etc.) bonds, greatly enriching aromatic chemistry and related fields. Some well known palladium–containing intermediates such as palladacycles and allylpalladium intermediates play an important role in organic

A facile and enantioselective approach to lactone‐fused chromanone derivatives from 1‐(2‐hydroxyaryl)‐1,3‐diketones and α,β‐unsaturated aldehydes under mild conditions has been developed, which included organocatalytic stepwise Michael addition/ cycloketalization/hemiacetalization and followed by oxidation reaction. In the presence of chiral amine organocatalyst and an additional salicylic acid, a

A visible‐light‐induced strategy to access sulfonated chromanes and sulfonated 1,2,3,4‐tetrahydroquinolines via a radical cascade cyclization of 1‐(arylethynyl)‐2‐(vinyloxy)benzenes and N‐allyl‐2‐(arylethynyl)anilines with aromatic and aliphatic sulfinic acids has been developed. In the presence of TBHP (7.5 mol%) as an oxidant and Eosin Y (3.0 mol%) as a photocatalyst, the reactions undergo smoothly

The enantioselective synthesis of chiral N,N‐acetals derived from α‐dicarbonyl compounds has been achieved. Good yields and enantioselectivities were observed for the reaction with various α‐dicarbonyl compounds with 2‐aminobenzamides using chiral bis(imidazoline)‐phosphoric acid catalysts. Based on these experimental investigations, a possible transition state is proposed to explain the origin of

In recent years, the transition‐metal catalyzed three‐component coupling of an aldehyde, an alkyne and an amine, commonly called A3 coupling have become a powerful tool in organic synthesis. The aim of this review is to give a general overview of A3 coupling utility in synthesis of heterocycles, highlighting the variety of compounds that can be directly accessed from single reactions. The diverse A3

Strong Brønsted acids were found to catalyze the oxidative condensation of 2‐aminothiophenols with aryl alkyl ketones in DMSO to provide a wide range of complex 2‐arylbenzothiazines. With acetophenones, dimeric 2‐arylbenzothiazines were formed. On the other hand, the reaction with propiophenones resulted in 2:1 adducts whereas 1:1 adducts were produced with isobutyrophenones, benzoylacetonitrile and

A synthetic strategy for the synthesis of substituted thiophenes is described by the one‐pot reaction of indoles with ketene dithioacetals under mild reaction conditions. Promoted by triflic acid (TfOH), the reaction of indoles with the easily available α‐acetyl ketene dithioacetals resulted in the formation of vinylketene dithioacetals via condensation instead of the well known nucleophilic addition‐alkylthio

The palladium‐catalyzed selective carbofunctionalization of inert γ‐C(sp3)‐O bonds of aliphatic amides by using the strategy of sp3 C‐H activation/β‐O elimination/hydrocarbofunctionalization with the assistance of 8‐aminoquinolyl directing group is presented here. This method features a broad scope of both 4‐hydroxypyridin‐2(1H)‐ones and 4‐hydroxy‐2H‐pyran‐2‐ones, providing a versatile method for the

The formation of hydrazinium salts by N‐N bond formation has typically involved the use of hazardous and difficult to handle reagents. Here, novel, mild and operationally simple conditions for the synthesis of hydrazinium salts are reported. Electrophilic nitrogen transfer to the nitrogen atom of tertiary amines, is achieved using iodosylbenzene as oxidant and ammonium carbamate as the N‐source. The