50916-19-3

Upstream product

• 103-82-2 phenylacetic acid 
• 536-90-3 m-Anisidine 
• 1228378-02-6 N-(3-methoxyphenyl)-2-oxo-2-phenylacetamide 
• 2398-37-0 3-methoxyphenyl bromide 
• 103-81-1 Benzeneacetamide 
• 2845-89-8 1-chloro-3-methoxy-benzene 
• 201230-82-2 carbon monoxide 
• 108-88-3 toluene 
• 103-80-0 phenylacetyl chloride 

Downstream Products

• 1371615-18-7 C₁₅H₁₃NO 
• 1371615-32-5 1-(4-(3-methoxyphenylamino)cyclopent-2-enyl)-2-phenylethanone 
• 33558-16-6 N-(3-methoxyphenyl)-N-(2-phenylethyl)amine 
• 1228378-02-6 N-(3-methoxyphenyl)-2-oxo-2-phenylacetamide 
• 85274-56-2 2-chloro-7-methoxy-3-phenylquinoline 

Relevant academic research and scientific papers

N-(Anilinoethyl)amide Melatonergic Ligands with Improved Water Solubility and Metabolic Stability

The MT2-selective melatonin receptor ligand UCM765 (N-(2-((3-methoxyphenyl)(phenyl)amino)ethyl)acetamide), showed interesting sleep inducing, analgesic and anxiolytic properties in rodents, but suffers from low water solubility and modest metabolic stability. To overcome these limitations, different strategies were investigated, including modification of metabolically liable sites, introduction of hydrophilic substituents and design of more basic derivatives. Thermodynamic solubility, microsomal stability and lipophilicity of new compounds were experimentally evaluated, together with their MT1 and MT2 binding affinities. Introduction of a m-hydroxymethyl substituent on the phenyl ring of UCM765 and replacement of the replacement of the N,N-diphenyl-amino scaffold with a N-methyl-N-phenyl-amino one led to highly soluble compounds with good microsomal stability and receptor binding affinity. Docking studies into the receptor crystal structure provided a rationale for their binding affinity. Pharmacokinetic characterization in rats highlighted higher plasma concentrations for the N-methyl-N-phenyl-amino derivative, consistent with its improved microsomal stability and makes this compound worthy of consideration for further pharmacological investigation.

Compound containing bipyrazole ring, intermediate thereof and application thereof

The invention discloses a compound containing a bipyrazole ring, and an intermediate and application thereof. The invention provides the compound containing a bipyrazole ring, as shown in a formula Iwhich is described in the specification. The compound can be used as a ligand, is high in selectivity, and is suitable for the application range of amide in C-N coupling and the C-C coupling reactionof arylboronic acid and aryl chloride, especially coupling with aryl chloride.

Preparation method of compound containing bipyrazole ring and intermediate thereof

The invention discloses a preparation method of a compound containing a bipyrazole ring and an intermediate of the compound. The preparation method of a bipyrazole ring-containing compound as shown ina formula I comprises the following steps: (1) adding alkali into a mixture of a bipyrazole ring compound as shown in a formula I-1 and a solvent for replacement reaction to obtain a mixed system; and (2) adding an organic phosphorus compound shown as a formula I-2 into the mixed system in the step (1), and carrying out a phosphonation reaction shown in the specification, so as to obtain the bipyrazole ring-containing compound shown as the formula I, wherein R1 and R2 are independently a C1-C6 alkyl group, a C3-C8 cycloalkyl group and a phenyl group, R3 is a C1-C6 alkyl group, and X is halogen. The prepared compound containing a bipyrazole ring can be used as a ligand, and is suitable for the application range of amide in C-N coupling and the C-C coupling reaction of arylboronic acid andaryl chloride.

Synthesis of α-ketoamides using potassium superoxide (KO2) as an oxidizing agent

A simple and convenient method for the synthesis of α-ketoamides by the oxidation of aryl acetamides using potassium superoxide (KO2) as an oxidizing agent is disclosed here. The scope of the developed method is successfully tested with fifteen substrates. In addition, the utility of method has been demonstrated by synthesizing an orexin receptor antagonist, a medicinally interesting compound.

Metal-free hydration of ynamides: Convenient approach to amides

The trifluoroacetic acid (TFA) mediated hydration of ynamides was developed, which is an efficient approach for the synthesis of N-monosubstituted amides. This convenient method is effective with a wide range of substrates under room temperature condition, and the products are obtained in high to excellent yields through an easy work-up process.

Chemoselective Reductive Deoxygenation and Reduction of α-Keto Amides by using a Palladium Catalyst

A palladium catalyst is used to synthesize 2,N-diphenylacetamides and α-hydroxy amides from readily available α-keto amides by chemoselective reductive deoxygenation and chemoselective reduction using polymethylhydrosiloxane (PMHS). This methodology has t

Amide bond formation via C(sp3)-H bond functionalization and CO insertion

An efficient method for the synthesis of amides via Pd-catalyzed oxidative carbonylation of C(sp3)-H bonds with CO and amines is described. The route efficiently provides substituted phenyl amides from alkanes.

Mesoporous Structured Silica - An improved catalyst for direct amide synthesis and its application to continuous flow processing

We recently published details of an effective, reusable and benign heterogeneous amidation catalyst based on thermal treatment of amorphous K60 silica, however the loading of catalyst required was high for some reactions. We report herein our further development of a series of heterogeneous catalysts based on structured silica (SBA) that retain all the green credentials of the previously described amorphous silica, but with increased efficiency. These catalysts were then utilised in continuous flow systems, achieving excellent conversions with dramatically reduced reaction times. ARKAT-USA, Inc.

Rapid in-plate generation of benzimidazole libraries and amide formation using EEDQ

A solution phase method for the preparation of etonitazene-related benzimidazoles and a general method for the preparation of amide derivatives in 96-well format have been developed for the generation of libraries of compounds in parallel.

ANALIDI AD ATTIVITA ANALGESICA ED ANTIPIRETICA

Several trimethylcyclopentyl and trimethylcyclopentenyl acetanilides, mono- and di-substituted on the aromatic nucleus as well as the corresponding acyl derivatives from aniline it self and corresponding phenylacetanilides, were prepared and tested as analgesics and antipyretics.Several compounds exhibit considerable activity in some cases superior to that of acetanilide.