90405-67-7

Upstream product

• 18925-69-4 N,N-dimethyl-2-phenylacetamide 
• 124-40-3 dimethyl amine 
• 50434-36-1 4-nitrophenylacetyl chloride 
• 7697-37-2 nitric acid 
• 98-95-3 nitrobenzene 
• 15722-62-0 N-Methyl-sarkosin-trimethylamid-Kation 
• 51738-10-4 2,2-dibromo-1-(4-nitrophenyl)ethene 
• 175658-07-8 N,N-dimethyl-thioglycolamide 
• 103-80-0 phenylacetyl chloride 
• 104-03-0 4-nitrobenzeneacetic acid 
• 555-16-8 4-nitrobenzaldehdye 

Downstream Products

• 5636-52-2 4-[2-(dimethylamino)ethyl]aniline 
• 81709-36-6 2-(4-Aminophenyl)N,N-dimethylacetamide 
• 861643-06-3 N,N-dimethyl-2-(4-nitrophenyl)ethanethioamide 
• 5339-05-9 N,N-dimethyl-2-(4-nitrophenyl)ethanamine 
• 539-15-1 N,N-dimethyltyramine 

Relevant academic research and scientific papers

ANTITUMOR-EFFECT ENHANCER USING PYRAZOLO[3,4-D]PYRIMIDINE COMPOUND

To provide a method for treating cancer using a pyrazolo[3,4-d]pyrimidine compound or a salt thereof. The present invention provides an antitumor agent comprising a pyrazolo[3,4-d]pyrimidine compound of formula (I) wherein X, Y, Z1, Z2/su

NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUND OR SALT THEREOF

To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 i

Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold

G protein-coupled receptors (GPCRs) represent a biological target class of fundamental importance in drug therapy. The GPRC6A receptor is a newly deorphanized class C GPCR that we recently reported for the first allosteric antagonists based on the 2-arylindole privileged structure scaffold (e.g., 1-3). Herein, we present the first structure-activity relationship study for the 2-arylindole antagonist 3, comprising the design, synthesis, and pharmacological evaluation of a focused library of 3-substituted 2-arylindoles. In a FRET-based inositol monophosphate (IP1) assay we identified compounds 7, 13e, and 34b as antagonists at the GPRC6A receptor in the low micromolar range and show that 7 and 34b display >9-fold selectivity for the GPRC6A receptor over related GPCRs, making 7 and 34b the most potent and selective antagonists for the GPRC6A receptor reported to date.

Synthesis and biological evaluation of new 4β-anilino-4′-O- demethyl-4-desoxypodophyllotoxin derivatives as potential antitumor agents

A series of new 4β-anilino-4′-O-demethyl-4-desoxypodophyllotoxin derivatives were prepared and evaluated for their cytotoxicities against four human cancer cell lines including KB, KB/VCR, A549 and 95D. Most compounds showed better growth-inhibition activities against tested cell lines than that of etoposide (VP-16). Preliminary structure-activity relationships (SARs) were concluded and it indicated that the side chains substituted at 4β position of podophyllotoxin significantly influenced the cytotoxic activity, especially for the drug resistance profile. In vivo studies of compound 26c on highly metastatic human lung cancer xenograft in nude mice showed that it can significantly inhibit tumor growth with administrating by oral route.

An efficient method for one-carbon elongation of aryl aldehydes via their dibromoalkene derivatives

Various aryl aldehydes were efficiently converted into one-carbon extended aryl acetamides or aryl acetic acids through the reaction of their dibromoalkene derivatives with pyrrolidine in the presence of water under very mild conditions.

Base-mediated reaction of quaternary ammonium salts with nitroarenes - Their useful functionalization via vicarious nucleophilic substitution (VNS)

Ammonium ylides generated from ammonium salt 1a-e with a base react with derivatives of 3-nitropyridine 2a-c and 2-nitrothiophene (3) to form products of vicarious nucleophilic substitution (VNS) 7, 8, or 9 respectively. The products of VNS 10, 11, or 12 are also produced from the corresponding ammonium salts, a base and 4-chloro-nitrobenzene (4), nitrobenzene (5), or 1-nitronaphthalene (6), respectively. In a few products, an exchange of alkoxy group 7c or substitution of chlorine by alkoxyl 8a,b occured.

Experiments on the Chaperon effect in the nitration of aromatics

A nitro group may be effectively delivered to the ortho position of alkylbenzenes, provided that a suitable chaperon function is located in α- position and a dilute of HNO3 in CH2Cl2 is used. The carbonyl function of an aldehyde or ketone is the best choice, but a carboxyl, alkoxycarbonyl, and amide groups all work well. The ether function showed a less pronounced ortho orientation effect, whereas the hydroxyl group was too prone to oxidation. Side reactions were minimal under the conditions employed. A para chaperon effect was seemingly at work in the CH2Cl2 nitration of benzenepropanenitrile. All the results were compared with the corresponding classical nitration in H2SO4.

Vicarious nucleophilic substitution of hydrogen proceeding via heterocyclic ring opening

Carbanions of five-membered S-heterocycles react with nitroarenes via the ring-opening VNS reaction or oxidative nucleophilic substitution of hydrogen. The reaction course is affected by rigidity of the ring.

Anticonvulsant activity of some 4-aminophenylacetamides

A series of 4-aminophenylacetamides was prepared and evaluated for anticonsulvant activity. These compounds were prepared during studies designed to determine the relationship between benzamide-like compounds and anticonsulvant effects. Unlike benzamides, these phenylacetamides have a methylene group between the aromatic ring and the amide carbonyl. Consequently, formal conjugation is lost, and the number of conformational degrees of freedom has increased. The compounds were tested in mice against seizures induced by electroshock and pentylenetetrazol, and in the rotorod assay for neurologic deficit. The more active and selective anticonsulvants prepared in this study were those having an additional aromatic ring as part of the substituent on the amide nitrogen. Compound 16, the 4-aminophenylacetamide derived from 2,6-dimethylaniline, was the most potent compound observed (ED50 = 50.50 mg/kg against electroshock-induced convulsions and ED50 = 93.20 mg/kg against pentylenetetrazol-induced convulsions).