A highly efficient HClO 4 catalysed substitutive phosphorylation of S‐, O‐ and N ‐based anthracene‐9‐ols with P(O)‐H species has been developed to afford phosphorylated 9,10‐dihydroanthracenes with a tetra‐ or trisubstituted carbon centre in good to excellent yields, which serves as a good complement to the established protocols that are limited to tertiary phosphorylated 9,10‐dihydroanthracenes. Gram‐scale

Diiodobenzenes were employed in palladium‐catalyzed one‐pot sequential reactions with propiolic acid and aryl halides to provide the corresponding diarylalkynyl benzenes. The combination of Pd(PPh 3 ) 4 (10 mol %) and DBU (5.0 equiv) gave optimal results in the sequence. Reactions with 1,2‐diiodobenzene gave higher yields than those utilizing 1,3‐ and 1,4‐diiodobenzenes. Furthermore, benzenes bearing

A highly efficient and simple procedure for the synthesis quinoline‐3‐carboxamides and their analogues via amidation reaction of quinoline‐3‐carboxylic acids with tetraalkylthiuram disulfides has been developed. The reaction proceeds efficiently under simple reaction conditions and features the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for

A novel and unprecedented route for the synthesis of pyrrolo[3,4‐c]quinoline N‐oxides is described. The synthetic approach involves a stepwise [3+2] cycloaddition/reductive cyclization from readily available 2‐nitrochalcones and activated methylene isocyanides. The unique feature of this transformation is the reductive cyclization of C−N bond forming without any external reductants. Moreover, the application

We report here a chemically synthetic method to introduce a PinB‐modified thymidine into well‐defined DNA first. The modification was designed to disturb the T‐A base‐pairing, thus regulate the DNA activity for PCR amplification . By treatment with small molecules, i.e., reactive oxygen species, the DNA polymerase activity was successfully restored. Due to tight temporal regulation and cell‐membrane

NiGa layered double oxide (Ni3Ga‐LDO) has been found to be an efficient heterogeneous catalyst for the α‐cyanation of aromatic tertiary amines using malononitrile as a low‐toxic cyanide source. Various aniline and aryltetrahydroisoquinoline derivatives were found to be tolerated by the catalytic system, and good to excellent yields for the corresponding products could be obtained. The results indicated

The benzothiadiazine 1,1‐dioxides were highly efficiently constructed via a BF 3 •Et 2 O promoted redox‐neutral cascade condensation/[1,7]‐hydride transfer/cyclization, which featured novel substrate skeletons, broad substrate scope, [1,7]‐hydride transfer manner, metal‐free conditions and the facile introduction of aryl, heteroaryl, allyl and propargyl groups etc.

Total synthesis of natural products often requires installation of double bond without adding carbon. Bamford‐Stevens and Shapiro reactions offer an option to execute such transformation. Several developments have been made in these reactions and their applications in a diverse area of chemistry. Lack of dedicated review on these reactions in recent time is hampering an access to collective information

Although different ways of converting 5‐(hydroxymethyl)furfural (1) to various substrates with high value have been sought, few transformations have obtained building blocks that can be very useful in the area of ​​fine chemistry. Herein, we report the synthesis of protoanemonin (5‐methylenefuran‐2(5H)‐one) from D‐fructose via compound (1), a versatile γ‐alkylidenebutenolide, using an efficient self‐catalysed

An efficient metal‐free approach has been devised towards the synthesis of azoles via C‐H insertion protocol. Various isocyanides were examined as effective C1‐synthons. The HFIP plays crucial role as hydrogen source and promoter of the reaction in order to reveal the maximum efficacies to accomplish the transformation in high yields of the products with excellent functional group tolerance. The control

The development of new methods for the direct synthesis of bioactive molecules is a pivotal topic in organic and medicinal chemistry. Herein, we describe the rhodium(III)‐catalyzed C–H functionalization of N ‐aryl phthalazinones with maleimides. The complete site‐selectivity and broad functional group tolerance are observed. Notably, this protocol allows the direct integration of phthalazinones and

Terminal alkynes were readily obtained via the reaction of alkynoic acids with N,N,N’,N’ ‐teramethylethylenediamine (TMEDA) in DMSO at 65 o C for 12 h. This method gave good yields and showed high functional group tolerance. In addition, deuterated terminal alkynes were formed in good yields when alkynoic acids were treated with D 2 O prior to the reaction with TMEDA.

Over the past few decades, thienoquinolines have gained considerable attention due to their biological and synthetic applications. Few reports have been disclosed on Thienoquinoline synthesis. Hence, in the present review, we provided a comprehensive update on the synthesis of Thienoquinolines. A brief description of the preparation procedure, reactivity, and mechanisms are included, where as possible

Complex, functionally embellished natural products embodying diverse, oxygen rich furofuranone fragments like furo[3,4‐ c ]furanone, furo[2,3‐ b ]furanone, furo[3,4‐ b ]furan‐2(3 H )‐one, furo[3,4‐ b ]furan‐4(2 H )‐one and furo[3,4‐ b ]furan‐6(4H)‐one as the key motif and displaying wide range of biological activities such as anti‐cancer, anti‐HIV, anti‐microbial activities, etc., continue to draw

Herein, a specialized review of the origin and state of the art of proline‐derived long‐aliphatic‐chain amphiphilic organocatalysts (PDLACAOs) and their use in asymmetric organic reactions in aqueous media (water, brine, and sea water), including in water and in the presence of water, is presented. The reactions in which they have been evaluated and the most important mechanisms are discussed.

A novel and efficient method has been developed for the synthesis of 2‐hydroxybenzoyl‐1 H ‐pyrazolylphosphonates and dihydrochromeno[3,2‐ c ]pyrazolylphosphonates by the reaction of 3‐formylchromones/3‐halo‐4 H ‐chromenones with Bestmann‐Ohira Reagent (BOR) in the presence of RuCl 3 catalyst. The reactions proceeded through decarbonylation, debromination, intramolecular cyclization and N ‐methylation

A metal‐free domino approach has been devised towards construction of two C‐S bonds for the synthesis of bioactive N, S‐heterocycles. The developed method was extended for the preparation of structurally diverse pyrazole tethered benzothiazole frameworks by using one‐pot operation of pyrazole C‐3/4/5 carbaldehydes, electron rich aromatic amines and elemental sulfur. This protocol provides excellent

A new Pd‐based catalytic system for the direct C–H arylation of arenes was developed. The use of a substoichiometric amount of quaternary ammonium salt as an additive with a Pd source achieved the direct arylation of unactivated arenes under milder reaction conditions in moderate to high yields. The ammonium salt generates the anionic palladium complex, thereby facilitating arylation by a concerted

2‐Amidobiphenyls are known to undergo intramolecular N–H arylation in presence of hypervalent iodine(III) reagents which lead to C–N coupling reaction. Herein, an unprecedented intermolecular C–C coupling reaction via carbenium ion over a nitrenium ion has been reported using sole oxidant PhI(OAc)2 suppressing the more facile intramolecular C‐N coupling.

An efficient palladium‐catalyzed intramolecular decarbonylative thioetherification of 2‐pyridyl thioesters to furnish 2‐pyridyl aryl or alkyl thioethers is reported. Notably, PdCl 2 /PPh 3 is found to be an effective catalytic system for decarbonylative thioetherification of 2‐pyridyl thioesters and is compatible under elevated temperature and strong basic conditions. This unique strategy is simple

The synthesis of symmetric biaryls via the iron‐catalyzed homo‐coupling of aryllithium reagents was developed under a mild condition, in the absence of ligand, with wide range of scope, and in good yields. Investigation on reaction concentration and practical utility of this environmentally friendly procedure also indicates a promising application outlook.

Light promoted two‐step one‐pot syntheses of quinoxalines and imidazo[1,2‐a]pyridines from alkynes and alkenes, respectively under mild conditions are described. The conversions occur via the formation of α,α’‐dibromoketones or α‐bromoketones on irradiation with LED (380‐390 nm) in acetonitrile/water mixture. This protocol does not require sensitizer or catalyst or additives. This two‐step protocol

We describe the Rh(I)‐catalyzed carbonylative [2+2+1] cycloaddition reactions of diynes with CO to give cyclopentadienone derivatives (CPDs). Previous reports on the use of neutral rhodium(I) complexes, such as [RhCl(cod)] 2 and RhCl(PPh 3 ) 3 , indicate that no CPD products are formed or that they are produced in low yields, even at elevated temperatures. The reaction described herein, which uses

Sulfoximine and its congeners are a versatile class of structural motifs widely found in a plethora of pharmaceutical compounds and crop protection industries due to their fascinating structural architecture. Former discoveries nicely demonstrates the synthetic routes of unmasked and various N‐functionalized sulfoximines but recent efforts from the synthetic community have divulged the applicability

Palladium‐catalyzed intramolecular cross‐dehydrogenative coupling of 3‐benzoyl substituted coumarins through C‒H activation is described to synthesize indeno[2,1‐c]chromene‐6,7‐diones. A broad range of indeno[2,1‐c]chromene‐6,7‐diones using this method could be easily achieved in moderate to good yields (up to 93%).

The activation and functionalization of C–H bonds using palladium catalysts has become an important part of a modern chemist toolbox, as it enables a range of highly useful transformations to be achieved in a single synthetic step. However, many established protocols for such C–H functionalizations rely on stoichiometric amounts of chemical oxidants, which are often expensive and/or toxic, and lower