85676-52-4

Upstream product

• 591-31-1 3-methoxy-benzaldehyde 
• 536-90-3 m-Anisidine 
• 79-11-8 chloroacetic acid 
• 62750-10-1 ethyl 2-((3-methoxyphenyl)amino)acetate 

Downstream Products

• 859980-67-9 N-(3-methoxy-phenyl)-N-nitroso-glycine 
• 261524-25-8 R,S-N-Methoxycarbonyl-2-(3-methoxyphenyl)-glycine 
• 1448616-14-5 (S)-tert-butyl 2-(2-((3-methoxyphenyl)amino)acetamido)-4-methylpentanoate 
• 1448616-36-1 (S)-N-((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)-2-(2-((3-methoxyphenyl)amino)acetamido)-4-methylpentanamide 
• 1610875-42-7 N-(4-bromo-3-methoxyphenyl)-2-(3-methoxyphenylamino)acetamide 
• 1610874-85-5 N-(3-methoxy-4-(1H-pyrazol-4-yl)phenyl)-2-(3-methoxyphenylamino)acetamide 
• 126689-77-8 methyl 2-(3-methoxyphenylamino)acetate 

Relevant academic research and scientific papers

Discovery and evolution of 12N-substituted aloperine derivatives as anti-SARS-CoV-2 agents through targeting late entry stage

So far, there is still no specific drug against COVID-19. Taking compound 1 with anti-EBOV activity as the lead, fifty-four 12N-substituted aloperine derivatives were synthesized and evaluated for the anti-SARS-CoV-2 activities using pseudotyped virus model. Among them, 8a exhibited the most potential effects against both pseudotyped and authentic SARS-CoV-2, as well as SARS-CoV and MERS-CoV, indicating a broad-spectrum anti-coronavirus profile. The mechanism study disclosed that 8a might block a late stage of viral entry, mainly via inhibiting host cathepsin B activity rather than directly targeting cathepsin B protein. Also, 8a could significantly reduce the release of multiple inflammatory cytokines in a time- and dose-dependent manner, such as IL-6, IL-1β, IL-8 and MCP-1, the major contributors to cytokine storm. Therefore, 8a is a promising agent with the advantages of broad-spectrum anti-coronavirus and anti-cytokine effects, thus worthy of further investigation.

Synthesis and evaluation of phenyl substituted sydnones as potential DPPH-radical scavengers

A series of phenyl substituted sydnones has been synthesized and their radical-scavenging activity has been studied on DPPH free radical. Out of eighteen compounds screened, nine compounds show interesting activity. A mechanism is presented whereby sydnones scavenge DPPH radical through donating H-atom at 4th-position. Its strong radical-scavenging activity mainly arises from 1, 2, 3-oxadiazolium-5-olate ring. Different substituents and their positions on the phenyl ring differently influence DPPH scavenging activity and therefore, may provide clues to design and develop better free-radical scavenging sydnones with multiple activities.

Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith

Method for the prevention or treatment of pruritis by administering to a patient an antipruritic compound, or pharmaceutically acceptable salt thereof, of the class arylacetamide, which is exemplified by compounds of the formulae I, II, IIA, III, IV and IVA having the structures: and in which R1-4, X, X4, X5, X7, X9, Y and Z are as described in the specification.

Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith

Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formula I, having the structure: wherein R1, R2; X; and Ar Y, Z and n are as described in the specification.

Production of an ester of one enantiomer of an α-amino acid in the form of a salt with an optically active acid

A process for the production of an ester of one enantiomer of an α-amino acid in the form of a salt with an optically active acid, which comprises reacting an ester of the opposite enantiomer of said α-amino acid (which may be in admixture with an ester of the desired enantiomer) with said optically active acid and an aldehyde or ketone, whereby an ester of the desired enantiomer separates out in the form of the said salt. The free α-amino acid and/or its salts may be obtained by hydrolysis of the ester thus formed. Optically active α-amino acids and their esters are of use in the synthesis of physiologically active compounds e.g. antibiotics of the penicillin and cephalosporin types. The present invention provides a relatively cheap, high yield process for the production of esters of optically active α-amino acids and for the production of optically active α-amino acids thereform. Certain novel compounds are disclosed.