57058-32-9

Upstream product

• 64-19-7 acetic acid 
• 89-97-4 2-CHLOROBENZYLAMINE 
• 7647-01-0 hydrogenchloride 
• 5027-32-7 1,1,2,2-Tetraacetylethan 
• 75-36-5 acetyl chloride 
• 108-24-7 acetic anhydride 
• 919-19-7 diethyl acetylphosphonate 
• 141-78-6 ethyl acetate 
• 60-35-5 acetamide 
• 89-98-5 2-chloro-benzaldehyde 

Downstream Products

• 80639-30-1 N-(2-Chloro-benzyl)-N-methyl-acetamide 
• 24331-94-0 1,4-dihydro-3(2H)-isoquinolinone 
• 4765-50-8 2-(2-chlorophenyl)quinazolin-4(3H)-one 

Relevant academic research and scientific papers

Dichotomy of Atom-Economical Hydrogen-Free Reductive Amidation vs Exhaustive Reductive Amination

Rh-catalyzed one-step reductive amidation of aldehydes has been developed. The protocol does not require an external hydrogen source and employs carbon monoxide as a deoxygenative agent. The direction of the reaction can be altered simply by changing the solvent: reaction in THF leads to amides, whereas methanol favors formation of tertiary amines.

Acetic acid as a catalyst for the N-acylation of amines using esters as the acyl source

We report a cheap and simple method for the acetylation of a variety of amines using catalytic acetic acid and either ethyl acetate or butyl acetate as the acyl source. Catalyst loadings as low as 10 mol% afforded acetamide products in excellent yields at temperatures ranging from 80-120 °C. The methodology can also be successfully applied for the synthesis of a broad range of other amides, including the formation of formamides at 20 °C.

An organocatalytic biomimetic approach to α-aminophosphonates

A novel biomimetic approach to optically active α-aminophosphonates utilizing readily available acylphosphonates and 2-chlorobenzylamine as starting materials has been described. The enantioselective protonation constitutes the main enantiodifferentiating step in the developed strategy. This nature-inspired approach proceeds efficiently and in a highly stereoselective manner. This journal is

H-β-zeolite catalyzed transamidation of carboxamides, phthalimide, formamides and thioamides with amines under neat conditions

Efficient transamidation of unactivated carboxamides, phthalimides, formamides and thioamides with amines under solvent-free conditions using H-β-zeolite as a green and recyclable heterogeneous catalyst is described. Easy work up, high purity of the products, recyclability and environmentally-friendly nature of the catalyst are the attractive features of the present methodology. This is the first report for the transamidation of thioamides under heterogeneous conditions.

An attractive route to transamidation catalysis: Facile synthesis of new o-aryloxide-N-heterocyclic carbene ruthenium(II) complexes containing trans triphenylphosphine donors

Well-defined robust ruthenium(II) complexes 3a-d bearing o-aryloxide-N-heterocyclic carbene ligands with different wingtip substituents (3a (R = Me), 3b (R = Ph), 3c (R = iPr) and 3d (R = Mes)) in the imidazole ring were synthesized in good yields by the reaction of imidazolium proligands with metal precursor [RuHCl(CO)(PPh3)3] by transmetallation from the corresponding silver carbene complexes. All the Ru(II)-NHC complexes have been characterized by elemental analyses, spectroscopic methods as well as ESI mass spectrometry. The molecular structure of the complex 3a was identified by means of single-crystal X-ray diffraction analysis, which revealed that the complexes possess a distorted octahedral geometry. In order to explore the catalytic potential of the synthesized complexes, all the four [Ru-NHC] complexes [3a-d] were tested as catalysts for transamidation of carboxamides with amines. Notably, the complex 3a was found to be very efficient and versatile catalyst toward transamidation of a wide range of amides with amines.

L-Proline: An efficient catalyst for transamidation of carboxamides with amines

In the presence of a catalytic amount of l-proline (10 mol %), transamidations of carboxamides with amines were achieved under solvent-free conditions. The transamidation process is compatible with a wide range of amines.

A novel and simple transamidation of carboxamides in 1,4-dioxane without a catalyst

An easy acylation and formylation of amines has been achieved via transamidation using 1,4-dioxane. The investigation works efficiently without an added catalyst and completes within short time under microwave irradiation.

Benzyl amide-ketoacid inhibitors of HIV-integrase

Integrase is one of three enzymes expressed by HIV and represents a validated target for therapy. Previous reports have demonstrated that the diketoacid-based chemotype is a useful starting point for the design of inhibitors of this enzyme. In this study, one of the ketone groups is replaced by a benzylamide resulting in a new potent chemotype. A preliminary SAR study is carried out to investigate the substitution requirements on the phenyl ring and methylene group of the benzylamide.

Synthesis of functionalized pyrroles by reaction of 3,4-diacetylhexane-2,5- dione with primary amines in water

3,4-Diacetylhexane-2,5-dione (tetra-acetylethane) undergoes a complex reaction with primary amines in boiling water to produce N-alkyl-3-acetyl-2,5- dimethylpyrroles, together with small quantities of N-alkyl-3,4-diacetyl-2,5- dimethylpyrroles and 2,5-dim

PROCESS FOR PRODUCING BENZYLAMINE DERIVATIVE

Disclosed is a process for producing a benzylamine derivative represented by the general formula (3): wherein X1, R1 and R2 are as defined below, which comprises reacting a benzyl derivative represented by the general form