Latest Articles of Synthesis | Chemsrc


Iridium-Catalyzed Regioselective Borylation of Substituted Biaryls 10.1055/s-0036-1591968 2018-03-28 Biarylboronic esters are generally prepared by directed ortho-metalation or by Miyaura borylation and hence rely on the presence of a directing group or pre-functionalization. In this paper, the preparation of biarylboronic esters by direct C–H borylation of...
CuI/Et2NH-Catalyzed One-Pot Highly Efficient Synthesis of 1,4-Disubstituted 1,2,3-Triazoles in Green Solvent Glycerol 10.1055/s-0036-1591557 2018-03-28 A concise one-pot three-component reaction of organic halides, terminal acetylenes, and sodium azide provided an efficient route for the synthesis of 1,2,3-triazoles. A variety of 1,2,3-triazoles were prepared in good to excellent yields with green solvent g...
Organocatalytic Electrochemical C–H Lactonization of Aromatic Carboxylic Acids 10.1055/s-0036-1591558 2018-03-28 An electrochemical strategy has been developed for radical arene carbon–oxygen bond formation. This reaction utilizes DDQ as a redox mediator, with inexpensive glassy carbon electrodes to facilitate an intramolecular lactonization of biphenyl-2-carboxylic aci...
Preparation of Trifluoromethylated (Arylaminomethylene)malononitriles Suitable for Synthesis of 4-Amino-2-(trifluoromethyl) quinoline Derivatives by Intramolecular Friedel–Crafts Reaction 10.1055/s-0037-1609433 2018-03-28 An approach for the synthesis of 4-amino-2-(trifluoromethyl)quinolines via the intramolecular Friedel–Crafts reaction of 2-(1-(arylamino)-2,2,2-trifluoroethylidene)malononitrile derivatives is reported. This simple protocol provides a wide variety of 4-amino-...
Catalyst-Free Synthesis of 3-(2-Quinolinemethylene)-Substituted Isoindolinones in Water 10.1055/s-0037-1609491 2018-03-28 A facile and environmentally benign approach toward the synthesis of novel 3-alkyl-substituted isoindolinones by three-component reactions of 2-formylbenzoic acids, primary amines and 2-methylazaarenes in water under catalyst- and additive-free conditions is...
Synthesis of Aryl Trifluoromethyl Ketones 10.1055/s-0036-1591971 2018-03-28 Trifluoromethyl ketones have recently been attracting considerable attention because they represent powerful synthetic building blocks with potential pharmaceutical applications. This short review provides an overview of recent development in the synthesis of...
Palladium-Catalysed Construction of All-Carbon Quaternary Centres with Propargylic Electrophiles: Challenges in the Simultaneous Control of Regio-, Chemo- and Enantioselectivity 10.1055/s-0036-1591957 2018-03-27 This article describes the palladium-catalysed three-component coupling of 1,3-dicarbonyl compounds with nucleophiles and propargylic electrophiles for the generation of quaternary all-carbon centres in a single step, which necessitates the simultaneous contr...
Stereoselective Allylation of Linear and Chiral β-Amino-α-Hydroxy Aldehydes: Total Syntheses of Tetraacetyl d-lyxo-, d-ribo-, and d-arabino-Phytosphingosines 10.1055/s-0037-1609343 2018-03-27 The stereoselective allylations of β-amino-α-hydroxy aldehydes are described. Several Lewis acids (BF3·OEt2, SnCl4, TiCl4, ZnCl2, and MgBr2·OEt2) were utilized in the allylations. The allylation of anti-β-NHCbz-α-OTBS substrate mediated by SnCl4 afforded th...
Synthesis of 1-Acyl-2-vinylcyclopropanes: Utilizing Copper-Carbenoid versus Sulfur Ylide Methodology 10.1055/s-0036-1591554 2018-03-27 The synthesis of a range of racemic 1-acyl-2-vinylcyclopropanes by using two different methodologies is studied. We have developed a copper-catalyzed process for converting diazoketones into 1-acyl-2-vinylcyclopropanes and a sulfur-ylide-mediated procedure w...
Unravelling Factors Affecting Directed Lithiation of Acylaminoaromatics 10.1055/s-0036-1591954 2018-03-27 Ureas, pivalamides, and carbamates are widely used as directing metalation groups (DMGs) due to their good directing ability, low cost, ease of access, and ease of removal. Lithiation of substituted benzenes having such directing metalation groups using vario...

Iridium-Catalyzed Regioselective Borylation of Substituted Biaryls

10.1055/s-0036-1591968

2018-03-28

Biarylboronic esters are generally prepared by directed ortho-metalation or by Miyaura borylation and hence rely on the presence of a directing group or pre-functionalization. In this paper, the preparation of biarylboronic esters by direct C–H borylation of...

CuI/Et2NH-Catalyzed One-Pot Highly Efficient Synthesis of 1,4-Disubstituted 1,2,3-Triazoles in Green Solvent Glycerol

10.1055/s-0036-1591557

2018-03-28

A concise one-pot three-component reaction of organic halides, terminal acetylenes, and sodium azide provided an efficient route for the synthesis of 1,2,3-triazoles. A variety of 1,2,3-triazoles were prepared in good to excellent yields with green solvent g...

Organocatalytic Electrochemical C–H Lactonization of Aromatic Carboxylic Acids

10.1055/s-0036-1591558

2018-03-28

An electrochemical strategy has been developed for radical arene carbon–oxygen bond formation. This reaction utilizes DDQ as a redox mediator, with inexpensive glassy carbon electrodes to facilitate an intramolecular lactonization of biphenyl-2-carboxylic aci...

Preparation of Trifluoromethylated (Arylaminomethylene)malononitriles Suitable for Synthesis of 4-Amino-2-(trifluoromethyl) quinoline Derivatives by Intramolecular Friedel–Crafts Reaction

10.1055/s-0037-1609433

2018-03-28

An approach for the synthesis of 4-amino-2-(trifluoromethyl)quinolines via the intramolecular Friedel–Crafts reaction of 2-(1-(arylamino)-2,2,2-trifluoroethylidene)malononitrile derivatives is reported. This simple protocol provides a wide variety of 4-amino-...

Catalyst-Free Synthesis of 3-(2-Quinolinemethylene)-Substituted Isoindolinones in Water

10.1055/s-0037-1609491

2018-03-28

A facile and environmentally benign approach toward the synthesis of novel 3-alkyl-substituted isoindolinones by three-component reactions of 2-formylbenzoic acids, primary amines and 2-methylazaarenes in water under catalyst- and additive-free conditions is...

Synthesis of Aryl Trifluoromethyl Ketones

10.1055/s-0036-1591971

2018-03-28

Trifluoromethyl ketones have recently been attracting considerable attention because they represent powerful synthetic building blocks with potential pharmaceutical applications. This short review provides an overview of recent development in the synthesis of...

Palladium-Catalysed Construction of All-Carbon Quaternary Centres with Propargylic Electrophiles: Challenges in the Simultaneous Control of Regio-, Chemo- and Enantioselectivity

10.1055/s-0036-1591957

2018-03-27

This article describes the palladium-catalysed three-component coupling of 1,3-dicarbonyl compounds with nucleophiles and propargylic electrophiles for the generation of quaternary all-carbon centres in a single step, which necessitates the simultaneous contr...

Stereoselective Allylation of Linear and Chiral β-Amino-α-Hydroxy Aldehydes: Total Syntheses of Tetraacetyl d-lyxo-, d-ribo-, and d-arabino-Phytosphingosines

10.1055/s-0037-1609343

2018-03-27

The stereoselective allylations of β-amino-α-hydroxy aldehydes are described. Several Lewis acids (BF3·OEt2, SnCl4, TiCl4, ZnCl2, and MgBr2·OEt2) were utilized in the allylations. The allylation of anti-β-NHCbz-α-OTBS substrate mediated by SnCl4 afforded th...

Synthesis of 1-Acyl-2-vinylcyclopropanes: Utilizing Copper-Carbenoid versus Sulfur Ylide Methodology

10.1055/s-0036-1591554

2018-03-27

The synthesis of a range of racemic 1-acyl-2-vinylcyclopropanes by using two different methodologies is studied. We have developed a copper-catalyzed process for converting diazoketones into 1-acyl-2-vinylcyclopropanes and a sulfur-ylide-mediated procedure w...

Unravelling Factors Affecting Directed Lithiation of Acylaminoaromatics

10.1055/s-0036-1591954

2018-03-27

Ureas, pivalamides, and carbamates are widely used as directing metalation groups (DMGs) due to their good directing ability, low cost, ease of access, and ease of removal. Lithiation of substituted benzenes having such directing metalation groups using vario...